Inhibiteurs et Agonistes des Voies Épigénétiques

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Epigenetics
Product Handbook

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Epigenetics
Epigenetic mechanisms include any process that alters gene function without changing the DNA sequence and are
mitotically and/or meiotically heritable. Many types of epigenetic processes have been identified, including DNA methylation,
alterations in the structure of histone proteins, and gene regulation by small non-coding RNAs.
Disruption of gene expression patterns controlled by epigenetics can lead to autoimmune diseases, cancer, and a variety of
other diseases. Enzymes such as HDACs and DNMTs involved in epigenetic inheritance serve as epigenetic targets with
numerous inhibitors already approved by the FDA, and many are undergoing clinical trials for the same purpose. Drugs that
inhibit DNA methylation or histone deacetylation (such as 5-azacitidine, Decitabine, and Vorinostat) have been studied for
the reactivation of tumor suppressor genes and repression of cancer cell growth[1]. The development of epigenetic drugs is
emerging as a promising way to treat these diseases[1].

DNMT inhibitors
5-Azacytidine
Decitabine
Zebularine

HDAC inhibitors
Vorinostat
Pracinostat
Nucleosome Panobinostat
Heterochromatin Valproic acid
gene promoter inaccessible HAT inhibitors
M Anacardic acid
PU139
M C646
A
A
Euchromatin
Easily
accessible
M
gene promoter A
M Euchromatin
A
Easily
accessible
KMT inhibitors gene promoter
EPZ-5676
EPZ-6438 KDM inhibitors
A-893 Namoline Histone tails
UNC 0638 Pargyline
IOX1
Chromosome Myricetin


Condensed section
of chromosome
Chromatin ?ber with packed nuclesome

DNA methytransferases (DNMT) Histone acetyltransferases (HAT) A Acetylation M Methylation

Lysine demethylases (KDM) Lysine methylthransferases (KMT) Histone deacetylases (HDAC)

Figure 1. Epigenetic targets[2].
CONTENTS
Histone Modifications 1 DNA methylation 5 Small non-coding RNA 7

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Inhibitors • Screening Libraries • Proteins
Histone Modifications
Histone modifications are able to alter chromatin structure and are associated with both transcriptional activation and
inhibition. Histone modifications can either activate or silence gene expression, depending on the residues added to the
targeted histones and the extent of the modification. There are various kinds of histone modifications, including acetylation,
methylation, citrullination, deamination, ubiquitination, and ADP-ribosylation.
Histone acetylation usually occurs on basic amino acids such as lysine and arginine. In general, acetylation activates gene
expression by reducing the affinity of histones to DNA. Histone acetylation is transfered by HATs and removed by HDACs.
HATs can be grouped into at least five subfamilies, including GNAT, MYST, p300/CBP, the general transcription factor HATs,
and the nuclear hormone-related HATs. CBP/p300 contains a bromodomain that is important in binding to chromatin, and
has attracted widespread attention as promising epigenetic targets for diverse human diseases[3].

Methylation, another widely studied histone modification, is catalyzed by histone methyltransferases. Histone methylation can
either activate or silence gene expression. For example, H3K4me3 activates gene expression, while H3K27me3 is associated
with gene silencing. Histone demethylation is performed by two classes of histone demethylases: lysine-specific demethylase
(LSD) family proteins (LSD1 and LSD2) and JmjC domain-containing histone demethylase (JHDM)[4].

Other histone modifications are relatively rare, including histone deamination/citrullination, ubiquitination, ADP-ribosylation,
N6-formylation, and O-GlcNAylation. For example, ADP-ribosylation of lysine residues occurs in less than 1% of histone
proteins, but is observed particularly in the case of single DNA strand breaks[5].

Enzymes that mediate histone modification marks (such as HATs) are known as "writers", while enzymes that remove these
modifications are called "erasers". In addition, some protein with domains have also been identified that can recognize specific
histone modifications (i.e., readers). For example, the bromodomains of BET proteins selectively target acetyllysine residues,
whereas JMJD2A and 53BP1 with tudor domains bind methylated arginines[6].
K
U
K —C
120
K
A
S
A
K M
T K P
A 15 20
K S K
S P U K 14
M
P A K A
12
5
A P
C— 120 M A
122 119
13
9 5 1
S
R
P R
T
M K K
M P K
2 2
M
3 R K
K A A
K K
3 4 M A K
K
A K K A 8 A R M
M
A
K M S T K
M 18 2327 M —C
A 9 P A 36 56
K A 5 P 17 79
A 10 14
12 8 11
M 16
C— 20

P Phosphorylation U Ubiquitination Histone H2A Histone H4 Histone H1

A Acetylation M Methylation Histone H2B Histone H3 DNA

Figure 2. Histone modifications[2].
MCE provide 1,000+ histone modifications related products, covering hot targets including HDACs, HATs, histone
demethylase, histone methyltransferase, PARP, BET proteins and others.
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Master of Bioactive Molecules

Compounds
Cat. No. Product Name Description Type
HY-100201 A-196 A selective inhibitor of SUV420H1 and SUV420H2, for the research of Methylation
the role of histone methyltransferases in genomic integrity.
HY-101451 PBIT A specific inhibitor of the JARID1 enzymes. Methylation
HY-102047B KDOAM-25 citrate A highly selective KDM5 inhibitor, increases global H3K4 methylation Methylation
at transcriptional start sites.
HY-10587 BIX-01294 A reversible and highly selective G9a and GLP Histone Methylation
Methyltransferase inhibitor
HY-112445 SGC3027 A histone methyltransferase inhibitor, the first selective and cell active Methylation
chemical probe for PRMT7.
HY-114208A BI-9321 A selective and cellular active nuclear receptor-binding SET domain 3 Methylation
trihydrochloride (NSD3)-PWWP1 domain antagonist.
HY-120137 CMP-5 A selective PRMT5 inhibitor, prevents EBV-driven B-lymphocyte Methylation
transformation but leaves normal B cells unaffected.
HY-12583 A-366 A highly selective, peptide-competitive histone methyltransferase G9a Methylation
inhibitor, and an inhibitor of the Spindlin1-H3K4me3-interaction.
HY-13643 Daminozide A plant growth regulator and KDM2/7 histone demethylases inhibitor. Methylation
HY-13807 UNC0646 A selective histone methyltransferase G9a and GLP inhibitor. Methylation
HY-13808 UNC 0631 A potent histone methyltransferase G9a inhibitor. Methylation
HY-15223 MI-3 A potent and high affinity menin-MLL inhibitor. Methylation
HY-15650 SGC0946 A selective DOT1LH3K79 methyltransferase inhibitor. Methylation
HY-W015114 L-2-Hydroxyglutaric Inhibits histone demethylases and hence promotes histone Methylation
acid disodium methylation, used in the research of renal cancer.
HY-100508 ITSA-1 A HDAC activator, counteracts Trichostatin A (TSA)-induced cell cycle Acetylation
arrest, histone acetylation, and transcriptional activation.
HY-100719 BRD-6929 A selective brain-penetrant inhibitor of HDAC1 and HDAC2, used for Acetylation
mood-related behavioral model research.
HY-101084 NSC 228155 An EGFR activator and an inhibitor of KIX-KID interaction, inhibits KID Acetylation
from CREB and KID-interacting domain (KIX) from CBP.

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Inhibitors • Screening Libraries • Proteins

Compounds
Cat. No. Product Name Description Type
HY-107569 Garcinol A histone acetyltransferases (HATs) and p300/CPB-associated factor Acetylation
inhibitor, has anti-inflammatory and anti-cancer activity.
HY-112789 (+)-JQ1 PA A BET inhibitor, with an IC50 of 10.4 nM. Acetylation
HY-128359 ACBI1 A cooperative SMARCA2, SMARCA4 and PBRM1 PROTAC degrader, Acetylation
induces apoptosis.
HY-128918 SIS17 A speific mammalian histone deacetylase 11 (HDAC 11) inhibitor. Acetylation
HY-13216 Pyroxamide A HDAC1 inhibitor induces apoptosis and cell cycle arrest. Acetylation
HY-15144 Trichostatin A A potent and specific inhibitor of HDAC class I/II. Acetylation
HY-15149 Romidepsin Inhibits HDAC1, HDAC2, HDAC4, and HDAC6, induces cell G2/M phase Acetylation
arrest and apoptosis.
HY-15489 Scriptaid A HDAC inhibitor, a sensitizer to antivirals and has potential for Acetylation
EBV-associated lymphomas research.
HY-15654 Sodium An inhibitor of HDAC and endoplasmic reticulum (ER) stress, used in Acetylation
4-phenylbutyrate cancer and infection research.
HY-15658 GSK2801 A selective, orally active and cell active acetyl-lysine competitive Acetylation
BAZ2A and BAZ2B bromodomains inhibitor.
HY-15815 Bromosporine A BET inhibitor arrests cell cycle and induces apoptosis in cancer cells. Acetylation
HY-15846 CPI-203 A potent and selective inhibitor of BET bromodomain. Acetylation
HY-16586 PFI-1 A selective BET inhibitor for BRD4. Acetylation
HY-19999A PF-CBP1 A highly selective inhibitor of the CREB binding protein bromodomain Acetylation
hydrochloride (CBP BRD), used for the research of neurological disorders.
HY-A0281 4-Phenylbutyric An inhibitor of HDAC and endoplasmic reticulum (ER) stress, used in Acetylation
acid cancer and infection research.
HY-N0005 Curcumin A natural phenolic compound, is a p300/CREB-binding protein-specific Acetylation
inhibitor of acetyltransferase.
HY-N6735 Apicidin A fungal metabolite, acts as a HDAC inhibitor, with antiparasitic Acetylation
activity and a broad spectrum antiproliferative activity.
HY-W013274 CPTH2 A HAT inhibitor, inhibits the histone H3 acetylation by Gcn5, decreases Acetylation
the invasiveness of a ccRCC cell line through the inhibition of KAT3B.

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Master of Bioactive Molecules

Compound Screening Libraries
Cat. No. : HY-L005 Cat. No. : HY-L024
Epigenetics Compound Library Histone Modi?cation Research Compound Library
A unique collection of 1,000+ epigenetics-related compounds. A unique collection of 500+ bioactive compounds targeting
Main targets: HDAC, Histone Demethylase, Histone Epigenetic Reader Domain.
Acetyltransferase (HAT), DNA Methyltransferase (DNMT), Main targets: HDAC, Histone Acetyltransferase, Sirtuin,
Epigenetic Reader Domain, MicroRNA, etc. Histone Demethylase, Histone Methyltransferase, etc.

Proteins, Peptides & Inhibitor Cocktail
Cat. No. Product Name Description Type
HY-P72336 Human/Xenopus laevis One of the five main histone proteins involved in the structure of Proteins
Histone H4 chromatin in eukaryotic cells.
HY-P76080 Human SMYD3 A member of the lysine methyltransferase family, plays an important Proteins
role in the methylation of histone non-histone targets.
HY-P72262 Human Histone HDACs play important roles in the regulation of gene expression, Proteins
deacetylase 1 apoptosis, stress responses, DNA repair, genomic stability.
HY-P71592 Mouse Sap130 May function in the assembly and/or enzymatic activity of mSin3A or Proteins
in mediating interactions between the complex and other regulatory
complexes.
HY-P75551 Human LSD1 Demethylates mono- and dimethyl-lysine on histone H3 to control Proteins
chromatin structure, resulting in transcriptional regulation.
HY-P2509 Histone H2A (1-20) A 35-residue a peptide of histone H2A, is a substrate for Peptides
methyltransferase/demethylase enzymes.
HY-P2258 Histone H3 (1-34) A peptide derived from human histone isotype 3.1. Histone variants Peptides
and histone modifications modulate chromatin structure, ensuring the
precise operation of cellular processes associated with genomic DNA.
HY-P2257 H3K4 (Me3) (1-20) A histone peptide. Trimethylation of H3K4 me3 is found in Peptides
active euchromatin but not in silent heterochromatin.
HY-P2480 Histone H1-derived A phosphopeptide and the peptide substrates contains a sequence in Peptides
Peptide accordance with the optimal recognition motif for CDKs.


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Inhibitors • Screening Libraries • Proteins

Cat. No. Product Name Description Type
HY-K0030 Deacetylase Inhibitor Deacetylase Inhibitor Cocktail is a synergistic combination of Inhibitor
Cocktail (100X) chemicals designed to preserve the acetylation state of proteins. Cocktail
HY-K0011 Protease Inhibitor Protease inhibitor cocktail is used in cell lysates or tissue extracts Inhibitor
Cocktail, mini-Tablet to increase protein stability. Cocktail
HY-K0013 Protease and Protease and Phosphatase Inhibitor Cocktail (EDTA-Free, 10× in Inhibitor
Phosphatase Inhibitor ddH2O) protects protein from degradation by endogenous Cocktail
Cocktail (EDTA-Free, 10× proteases released during protein extraction and purification.
in ddH2O)
DNA Methylation
DNA methylation is a common epigenetic alteration and considered a heterochromatin mark. DNA methylation plays an
important role in maintaining the stability of genome, genomic imprinting, X-chromosome inactivation in females, regulation
of transcription, and also in the developmental process of an organism[2].

DNA methylation modifications include 5-methylcytosine (5mC), N6-methylladenine (6mA) and 4-methylcytosine (4mC).
Among them, 6mA and 4mC are prevalent in prokaryotic genomes, 5mC is the most widely distributed type of methylation in
eukaryotes. DNA methyltransferases (DNMTs) target CpG sites and actively methylate DNA. DNMT3A/B are the “de novo”
DNMTs and transfer methyl groups onto naked DNA (Figure 3a). However DNMT1 preserves preexisting pattern of methylation
after cell replication (Figure 3b)[4][7]. DNA methylation is recognized by three separate families of proteins: the MBD
(methyl-CpG-binding domain) proteins, the UHRF (ubiquitin-like, containing PHD and RING finger domain) proteins, and the
zinc-finger proteins[7].
a b 3’ 3’
CH 3
T T G A C A G C C G T 5’ 5’
5’ 3’
3’ 5’
A A C T G T C G G C A CH 3

Dnmt3a T T G A C A G C C G T T T G A C A G C C G T A A C T G T C G G C A A A C T G T C G G C A Dnmt3b
5’ Dnmt1 5’
3’ 3’
CH
3
T T G A C A G C C G T
5’ 3’
3’ 5’
A A C T G T C G G C A A A C T G T C G G C A T T G A C A G C C G T T T G A C A G C C G T
3’ A A C T G T C G G C A 3’
5’ 5’
Figure 3. DNA methylation pathways[3].

DNA demethylation is characterized as either passive or active. The inhibition or dysfunction of DNMTs allows newly incorporated
cytosine to remain unmethylated and consequently reduces the overall methylation level following each cell division.
Active DNA demethylation requires enzymes such as activation-induced cytidine deaminase (AID) and ten-eleven translocation
(TET) enzymes to process 5mC in order to revert it back to a naked cytosine[4].
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Master of Bioactive Molecules

MCE offers 100+ compounds related to DNA methylation, covering various targets including DNMTs, TET enzymes, cytidine
deaminase, UHRF proteins, MBD proteins, EZH2, and others.

Compounds
Cat. No. Product Name Description Type
HY-101925 CM-272 A selective and reversible dual G9a/DNA methyltransferases Methylation
(DNMTs) inhibitor with antitumor activities.
HY-103236 NSC232003 A highly potent UHRF1 inhibitor, which inhibits DNA methylation Methylation
in vitro and disrupts DNMT1/UHRF1 interactions.
HY-103397 Nanaomycin A A quinone antibiotic and the first selective DNMT3B inhibitor, with Methylation
anti-tumor and anti-parasite activity.
HY-10586 5-Azacytidine A nucleoside analogue of cytidine that specifically inhibits DNA Methylation
methylation, induces cell autophagy.
HY-116217 5-Fluoro- A tumor-selective prodrug of the potent thymidylate synthase Methylation
2'-deoxycytidine inhibitor 5-fluoro-2?-dUMP (a DNMT inhibitor).
HY-125292 NV03 A selective antagonist of UHRF1- H3K9me3 interaction by binding Methylation
to UHRF1 tandem tudor domain.
HY-12746 DC-05 A DNA methyltransferase 1 (DNMT1) inhibitor. Methylation
HY-12747 DC_517 A DNA methyltransferase 1 (DNMT1) inhibitor. Methylation
HY-13057 O6BTG- A potent O6-methylguanine-DNAmethyl-transferase (MGMT) inhibitor. Methylation
octylglucoside
HY-13420 Zebularine A DNA methyltransferase inhibitor, inhibits cytidine deaminase. Methylation
HY-13642 RG108 A non-nucleoside DNA methyltransferases (DNMTs) inhibitor causes Methylation
demethylation and reactivation of tumor suppressor genes.
HY-13668 Lomeguatrib A potent O6-methylguanine-DNAmethyl-transferase (MGMT) inhibitor. Methylation
HY-13962 SGI-1027 A DNA methyltransferase (DNMT) inhibitor, induces apoptosis. Methylation
HY-103236 NSC232003 A potent UHRF1 inhibitor, inhibits DNA methylation in vitro and Methylation
disrupts DNMT1/UHRF1 interactions.
HY-131031 KCC-07 A selective and brain-penetrant MBD2 (methyl-CpG-binding domain Methylation
protein 2) inhibitor, prevents binding of MBD2 to methylated DNA.
HY-144904 MC4343 A potent and dual inhibitor of EZH2 and HDAC. Methylation

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Inhibitors • Screening Libraries • Proteins

Compounds
Cat. No. Product Name Description Type
HY-A0004 Decitabine An orally active deoxycytidine analogue antimetabolite and a DNA Methylation
methyltransferase inhibitor, with anti-cancer activity.
HY-B2194 ?-Oryzanol Significantly inhibits the activities of DNMT1, DNMT3a. Methylation
HY-B2230 Hinokitiol Reduces Nrf2 expression, decreases DNMT1 and UHRF1 mRNA and Methylation
protein expression, with anti-infective, and anti-tumor activities.
HY-129079A TFMB-(S)-2-HG A potent inhibitor of the 5'-methylcytosine hydroxylase TET2, also Demethylation
inhibits the EglN prolyl hydroxylases.
HY-113038B ?-Hydroxyglutaric Inhibits multiple ?-ketoglutarate-dependent dioxygenases, including Demethylation
acid histone demethylases and the TET family of 5mC hydroxylases.
HY-15345 Tetrahydrouridine A potent inhibitor of cytidine deaminase (CDA). Demethylation
dihydrate
HY-120395 UC-514321 Directly targets STAT3/5 and represses TET1 expression. Demethylation
Small non-coding RNAs (ncRNAs)
In the 1990s, it was found that small double-stranded RNAs (dsRNAs) were able to mediate post-transcriptional gene
silencing of complementary mRNAs in the nematode Caenorhabditis elegans through a process called RNA interference
(RNAi). This discovery led to the realization that small ncRNAs are key regulators of gene expression in many different cellular
pathways and systems. MicroRNAs (miRNAs) and endogenous small interfering RNAs (siRNAs) are the most thoroughly
investigated non-coding RNAs[8].

SiRNA is a small exogenous dsRNA (~20 nts), which triggers the RNAi pathway. It unwinds and the sense strand is degraded.
The antisense strand forms an RNA-induced silencing complex (RISC) with various protein components. The antisense
strand retained in RISC is specifically complementary to the target gene mRNA. Meanwhile, RISC can cut and degrade the
target mRNA, inhibiting the target gene expression. Incomplete complementarity results in mRNA translation inhibition[9].

MiRNAs are highly evolutionarily conserved and small single-stranded ncRNAs (~22 nts). The primary mode of action for
miRNA and siRNA is similar; both form RISC complexes that trigger endogenous RNAi by regulating the stability or inducing
mRNA degradation. However, miRNAs usually bind to the 3'-UTR of mRNA. For mammals, the base pairing is always
imperfect, resulting in suppression of mRNA translation[10]. Meanwhile, plant miRNAs bind with near-perfect complementarity
to sites within the coding sequence of their targets, and the mRNA of target genes is sliced and degraded[11].

Currently, the utilization of small ncRNAs as drugs has become a relatively novel approach compared to conventional small
molecule inhibitors. The recent FDA approvals of Givosiran, Lumasiran, and Viltolarsen have ushered in the wave of RNAi or
RNA-based therapies into the mainstream of drug development. The potential of RNA therapies in precision genetics has
raised enthusiasm for similar applications in cancer, cardiovascular diseases, and rare disease therapies[12].
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Master of Bioactive Molecules

Gene
5’ Cap Transcription Transcription
dsRNA
Pri-miRNA
AAAAAAAA DGCR8
Rnase III enzymes
Drosha


Pre-miRNA
Ran-GTP SID-1
Transmembrane protein
Transmembrane protein
Exportin 5

Pre-miRNA dsRNA
RNase III DCR-1
enzyme Dicer

siRNA
miRNA—miRNA* duplex RISC Argonaute protein
RNase III siRNA binds RISC
enzyme
RISC

Mature miRNA siRISC
RISC
miRNA binds RISC siRNA unwinding
Argonaute protein
RISC
RISC
Activated RISC
Association with
target mRNA mRNA
Association with
target mRNA mRNA
RISC
RISC

Translational Target mRNA cleavage
repression
A G
Target mRNA degradation U
U C A
miRNA pathway siRNA pathway

Figure 4. Formation mode and regulatory mechanisms of miRNA and siRNA[9].

MCE offers 4,000+ compounds related to Non-coding RNAs, including miRNAs, siRNAs, liposome for siRNA delivery,
antisense oligonucleotide (ASO), and others.

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Inhibitors • Screening Libraries • Proteins

Compounds
Cat. No. Product Name Description Type
HY-132588 Lumasiran Inhibits the synthesis of oxalate, which is the toxic metabolite that is siRNA
directly associated with the clinical manifestations of PH1.
HY-132591 Inclisiran Inhibits PCSK-9 transcription, for cardiovascular disease research. siRNA
HY-132596 Tivanisiran A siRNA was designed to silence TRPV1, used for the study of dry eye siRNA
disease.
HY-132610 Givosiran A siRNA that targets hepatic ALAS1 messenger RNA, used for the siRNA
research of acute intermittent porphyria.
HY-108753 Eteplirsen Targets exon 51 in defective gene variants, used for Duchenne muscular ASO
dystrophy research.
HY-112980 Nusinersen Modifies pre-messenger RNA splicing of the SMN2 gene and thus ASO
promotes increased production of full-length SMN protein.
HY-132586 Viltolarsen Targets the splicing of exon 53 in the dystrophin gene used for the ASO
research of the Duchenne muscular dystrophy (DMD).
HY-132600 RG-101 Antagonizes miR-122. miR-122 is an important host factor for hepatitis C ASO
virus (HCV) replication.
HY-132608 Inotersen sodium Targets the TTR transcript and reduces the TTR mRNA levels, for the ASO
research of hereditary TTR amyloidosis polyneuropathy.
HY-132611 Golodirsen Specifically targets exon 53 of dystrophin pre-mRNA, used for the ASO
research of Duchenne muscular dystrophy (DMD).
HY-139290 RGLS4326 A first-in-class, short oligonucleotide miR-17 inhibitor, for the research of ASO
autosomal dominant polycystic kidney disease (ADPKD).
HY-143230 Custirsen A clusterin inhibitor, an antiapoptotic protein that is upregulated in ASO
response to chemotherapy and that confers treatment resistance.
HY-145729 Danvantisen An antisense oligonucleotide for STAT3 with antitumor activity. ASO
HY-150724 ODN 1018 A TLR-9 agonist, used as a vaccine adjuvant. CpG ODN
HY-150741 ODN 2216 A TLR-9 agonist, induces IFN-?/IFN-?, used as a vaccine adjuvant. CpG ODN
HY-135276 Targaprimir-96 Inhibits miR-96 processing, selectively modulates miR-96 production in Small
cancer cells and triggers apoptosis. Molecule


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Master of Bioactive Molecules

Compounds
Cat. No. Product Name Description Type
HY-15861 Targapremir-210 A selective miR-210 inhibitor. Targapremir-210 inhibits Small
pre-miR-210 processing with high binding affinity. Molecule
HY-112005 DOPE A neutral helper lipid for cationic liposome, improves transfection Lipid
efficiency of naked siRNA.
HY-112251 D-Lin-MC3-DMA An ionizable cationic lipid, is a potent siRNA delivery vehicle. Lipid
HY-130751 DODAP A cationic lipid, used to encapsulate siRNA. Lipid
HY-134541 SM-102 An ionizable amino lipid, used for the formation of LNPs. Lipid
HY-145795 OF-02 An alkenyl amino alcohol (AAA) ionizable lipid for highly potent in vivo Lipid
mRNA delivery.
HY-N0322 Cholesterol The major sterol in mammals, makes up 20-25% of structural compo- Lipid
nents of the plasma membrane.
HY-W040193 DSPC A cylindrical-shaped lipid, used to synthesize liposomes, and Lipid
is the lipid component in the lipid nanoparticle (LNP) system.
HY-138300 ALC-0159 A polyethylene glycol (PEG) lipid conjugate, could be used as vaccine Lipid
excipient.


References:
[1] Crit Rev Oncol Hematol. 2017;111:166-172 [2] Pharmacol Ther. 2017;173:118-134. [3] Eur J Med Chem. 2021;209:112861.
[4] Genet Epigenet. 2016;8:43-51. [5] Cold Spring Harb Perspect Biol. 2016;8(4):a019521. [6] Cold Spring Harb Perspect Biol. 2014;6(7):a018762.
[7] Neuropsychopharmacology. 2013;38(1):23-38. [8] Adv Exp Med Biol. 2016;937:3-17. [9] J Zhejiang Univ Sci B. 2018;19(10):739-749.
[10] J Cell Physiol. 2019;234(5):5451-5465. [11] Cell. 2009;136(4):642-655. [12] Mol Cancer. 2021;20(1):54.


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 Publications Citing Use of MCE Products Nature. 2020 Apr;580(7803):386-390.
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 Table of Contents Signaling Pathways
PI3K/Akt/mTOR 1
Epigenetics 1
Autophagy 2
Apoptosis 2
Cell Cycle/DNA Damage 3
Metabolic Enzyme/Protease 4
Protein Tyrosine Kinase/RTK 5
Immunology/Inflammation 6
Stem Cell/Wnt 6
Anti-infection 7
JAK/STAT Signaling 8
MAPK/ERK Pathway 8
GPCR/G Protein 9
Neuronal Signaling 10
Membrane Transporter/Ion Channel 11
Cytoskeleton 12
NF-?B 12
TGF-beta/Smad 13
VD/VDR 13
Antibody-drug Conjugate/ADC Related 14
PROTAC 15

Compound Screening Libraries 16
Virtual Screening 19
Dye Reagents 22

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Inhibitors • Agonists • Screening Libraries
PI3K/Akt/mTOR
Akt AMPK Cat. No. Product Name Cat. No. Product Name
ATM/ATR DNA-PK HY-10219 Rapamycin (Sirolimus) HY-13003 Torin 1
GSK-3 MELK HY-15244 Alpelisib HY-15186 Ipatasertib (GDC-0068; RG7440)
mTOR PDK-1 HY-19312 3-Methyladenine (3-MA) HY-13522 Fimepinostat (CUDC-907)
PI3K PI4K HY-10182 CHIR-99021 HY-70063 Buparlisib (BKM120)
PIKfyve PTEN HY-10108 LY294002 HY-13002 Torin 2
HY-10358 MK-2206 HY-13417 AICAR
HY-19323 Ceralasertib (AZD6738) HY-101566A BAY-1895344
HY-12513 LY3023414 HY-P0175 740 Y-P
HY-10218 Everolimus (RAD001) HY-10422 AZD-8055
HY-101562 GDC-0077 HY-13026 Idelalisib (CAL-101; GS-1101)
HY-101570 Nedisertib HY-19939S VX-984
HY-15346 Copanlisib HY-10514 BX795
HY-13902 Berzosertib (VE-822; VX-970) HY-15512A OTSSP167
HY-15431 Capivasertib (AZD5363) HY-13074 VO-Ohpic
HY-17471A Metformin HY-12046 PIK-93
Epigenetics
AMPK Cat. No. Product Name Cat. No. Product Name
Aurora Kinase HY-13030 (+)-JQ-1 HY-15149 Romidepsin (FK 228)
DNA Methyltransferase HY-15743 Birabresib (OTX-015; MK-8628) HY-15145 SRT 1720
Epigenetic Reader Domain HY-13803 Tazemetostat (EPZ-6438) HY-12635 SP2509
HDAC HY-13470 GSK126 HY-108696 GNE-781
Histone Acetyltransferase HY-107455 A-485 HY-A0004 Decitabine (5-Aza-2'-deoxycytidine)
Histone Demethylase HY-104048 QC6352 HY-13980 UNC0642
Histone Methyltransferase HY-101563 GSK3326595 HY-15452 Selisistat (EX-527)
JAK HY-15144 Trichostatin A (TSA) HY-111048 Corin
MicroRNA HY-15229 Guadecitabine (SGI-110) HY-13235 I-BET151
PARP HY-13032 Molibresib (I-BET762; GSK525762) HY-100482 CPI-637
PKC HY-103713 Seclidemstat (SP-2577) HY-12186 3-Deazaneplanocin A (DZNep)
Protein Arginine Deiminase HY-13418 Dorsomorphin (Compound C) HY-100514 GSK484
Sirtuin HY-15648B GSK-J4 HY-16425 RG2833
HY-101564 JNJ-64619178 HY-12163 Entinostat (MS-275)
HY-16925 MI-503 HY-10224 Panobinostat (LBH589)
1

 MCE
Master of Small Molecules
Autophagy
Autophagy FKBP Cat. No. Product Name Cat. No. Product Name
LRRK2 Mitophagy HY-11109 Resatorvid (TAK-242) HY-10971 Alisertib (MLN8237?
ULK HY-10162 Olaparib (AZD2281) HY-B0015 Paclitaxel (Taxol)
HY-100411 MLi-2 HY-17559 Actinomycin D
HY-70002 Enzalutamide (MDV3100) HY-17394 Cisplatin (CDDP)
HY-B0146 Verteporfin HY-15371 Forskolin (Coleonol)
HY-13756 Tacrolimus (FK506; Fujimycin) HY-17371 Oxaliplatin
HY-13992 AP20187 HY-13636 Fulvestrant (ICI 182780)
HY-13259 MG-132 HY-12481 SAR405
HY-19312 3-Methyladenine (3-MA) HY-100006A MRT68921
HY-13251 Silvestrol HY-16966 SBI-0206965
HY-12320 Cycloheximide (Actidione; CHX) HY-13018 MRT67307
HY-10108 LY294002 HY-100941 CCCP
HY-15142 Doxorubicin HY-16592 Brefeldin A (BFA)
HY-100558 Bafilomycin A1 HY-12990 Spautin-1
HY-50856 Ruxolitinib (INCB18424) HY-10129 Veliparib (ABT-888)
Apoptosis
Apoptosis Bcl-2 Family Cat. No. Product Name Cat. No. Product Name
c-Myc Caspase HY-100741 S63845 HY-100579 Ferrostatin-1
DAPK Ferroptosis HY-10087 Navitoclax (ABT-263) HY-16046 Rimiducid (AP1903)
FKBP IAP HY-13756 Tacrolimus (FK506; Fujimycin) HY-F0003 NADPH
MDM-2/p53 PKD HY-13992 AP20187 (B/B Homodimerizer) HY-101565 AMG-176
RIP Kinase Survivin HY-16658 Z-VAD(OMe)-FMK HY-101297 Z-IETD-FMK
Thymidylate Synthase HY-15763 Erastin HY-18658 Siremadlin (HDM 201)
TNF Receptor HY-13205 Belnacasan (VX-765) HY-19741 A-1331852
HY-15676 Idasanutlin (RG7388) HY-12466 Z-DEVD-FMK
HY-114481 Imidazole ketone erastin (IKE) HY-102080 SAFit2
HY-12296 AMG 232 HY-12726 Liproxstatin-1
HY-50936 Trabectedin (ET-743) HY-12635 SP2509
HY-15531 Venetoclax (ABT-199; GDC-0199) HY-13002 Torin 2
HY-12305 Q-VD-OPh (QVD-OPH? HY-50907 ABT-737
HY-15518 LCL161 HY-16591 Birinapant
HY-10959 RG7112 HY-10396 Emricasan (PF 03491390)
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Inhibitors • Agonists • Screening Libraries
Cell Cycle/DNA Damage
Antifolate Cat. No. Product Name Cat. No. Product Name
APC HY-13631A Exatecan HY-16592 Brefeldin A (BFA)
ATM/ATR HY-13442A Eribulin Mesylate HY-12137 Volasertib (BI 6727)
Aurora Kinase HY-10162 Olaparib (AZD2281) HY-16209 Forodesine (BCX-1777)
Casein Kinase HY-10619 Niraparib (MK-4827) HY-101212 CYC065
CDK HY-114177 PF-06873600 HY-103618 THZ531
Checkpoint Kinase (Chk) HY-16737 Elafibranor (GFT505) HY-13624A Epirubicin (4'-Epidoxorubicin)
CRISPR/Cas9 HY-15162 Monomethyl auristatin E (MMAE) HY-50855 Silmitasertib (CX-4945)
Deubiquitinase HY-13251 Silvestrol HY-50935 Troglitazone (CS-045)
DNA Alkylator/Crosslinker HY-12320 Cycloheximide (Actidione; CHX) HY-17371 Oxaliplatin
DNA-PK HY-16297 Abemaciclib (LY2835219) HY-104044 Pamiparib (BGB-290)
DNA/RNA Synthesis HY-10993 Adavosertib (AZD1775; MK-1775) HY-16261 Aldoxorubicin (INNO-206)
Eukaryotic Initiation Factor (eIF) HY-10617 Rucaparib (AG-014699) HY-80013 THZ1
G-quadruplex HY-50767 Palbociclib (PD 0332991) HY-101566A BAY-1895344
Haspin Kinase HY-13316 Mitomycin C (Ametycine) HY-112162 BOS-172722
HDAC HY-19323 Ceralasertib (AZD6738) HY-10129 Veliparib (ABT-888)
HSP HY-103712A Samuraciclib (CT7001) HY-12214A NVP-2
IRE1 HY-112088 AZD4573 HY-13469 Debio 0932 (CUDC-305)
Kinesin HY-16106 Talazoparib (BMN-673) HY-19831 4EGI-1
LIM Kinase (LIMK) HY-17565 Bleomycin HY-13753 Streptozocin (Streptozotocin)
Microtubule/Tubulin HY-112654 GCN2iB HY-B0779 Teprenone (Geranylgeranylacetone)
Mps1 HY-10971 Alisertib (MLN 8237) HY-12871B Atuveciclib (BAY-1143572)
Nucleoside Antimetabolite/Analog HY-12037 Rigosertib (ON-01910) HY-15372 GW 6471
p97 HY-B0015 Paclitaxel (Taxol) HY-114258 LY3295668 (AK-01)
PAK HY-17559 Actinomycin D HY-90006 5-Fluorouracil (5-FU)
PARP HY-104040 MKC8866 HY-30237 Seliciclib (Roscovitine; CYC202)
PERK HY-19620 Branaplam (LMI070) HY-15725 CDDO-Im (RTA-403)
Polo-like Kinase (PLK) HY-17394 Cisplatin (CDDP) HY-100888 Simurosertib (TAK-931)
PPAR HY-101570 Nedisertib (M3814) HY-18682 Centrinone (LCR-263)
RAD51 HY-10211 Tanespimycin (17-AAG) HY-18072 GSK2606414
ROCK HY-13902 Berzosertib (VE-822; VX-970) HY-17618 Pemafibrate
Sirtuin HY-15777 Ribociclib (LEE011) HY-107986 GNE-6776
SRPK HY-109101 Risdiplam (RG7916; RO7034067) HY-12861 CB-5083
Telomerase HY-18174 Prexasertib (LY2606368) HY-130250 SR-4835
TOPK HY-17364 Temozolomide (TMZ) HY-15147 XAV-939
Topoisomerase HY-10492 Dinaciclib (SCH 727965) HY-13323 CX-5461
3

 MCE
Master of Small Molecules
Metabolic Enzyme/Protease
Oxidoreductases: Elastase Cat. No. Product Name Cat. No. Product Name
5 alpha Reductase Factor Xa HY-12248 Telaglenastat HY-10227 Bortezomib
5'-Deiodinase Glucosidase HY-12222 Obeticholic acid HY-N0565B Doxycycline
Aldehyde Dehydrogenase MAGL HY-16901 Firsocostat HY-101560 Linrodostat
Aldose Reductase MMP HY-13756 Tacrolimus HY-14434 Asunaprevir
Cytochrome P450 Neprilysin HY-70062 Pevonedistat HY-15193 EMD638683
Dopamine ?-hydroxylase Phosphatase HY-13259 MG-132 HY-P0025 NIM811
Glutathione Peroxidase Phosphodiesterase (PDE) HY-19312 3-Methyladenine HY-B0764 Bucladesine
HIF/HIF Prolyl-Hydroxylase Phospholipase HY-12219A MSI-1436 HY-100116A Mitoquinone
HMG-CoA Reductase Proteasome HY-15689 Epacadostat HY-13426 Roxadustat
Indoleamine 2,3-Dioxygenase Renin HY-12867 PT-2385 HY-120384 AZD-0284
Isocitrate Dehydrogenase Soluble Epoxide Hydrolase HY-109083 Cilofexor HY-50876 (E)-Daporinad
Lactate Dehydrogenase Thrombin HY-18657 TEPP-46 HY-112929 DT-061
Lipoxygenase Lyases: HY-116009 RMC-4550 HY-108697 PT2399
NADPH Oxidase Carbonic Anhydrase HY-101979A CB-1158 HY-50108 GW 4064
Stearoyl-CoA Desaturase Decarboxylase HY-15424 5-Iodotubercidin HY-17367A Atazanavir
Tryptophan Hydroxylase Enolase HY-107418 Tropifexor HY-17605 Bictegravir
Tyrosinase Ligase: HY-12434 INT-767 HY-13966 2-Deoxy-D-glucose
Xanthine Oxidase Acetyl-CoA Carboxylase HY-15676 Idasanutlin HY-D0937 Methoxy-PMS
Transferases: Isomerase HY-12296 AMG 232 HY-18767 Ivosidenib
COMT Others: HY-100388 SHP099 HY-14771A Imeglimin
Acyltransferase CETP HY-18770B Navoximod HY-10502 Tipifarnib
Carbohydrate transferase Drug Metabolite HY-112645 BAY-2402234 HY-15287A Nelfinavir
E1/E2/E3 Enzyme Endogenous Metabolite HY-101842 ND-646 HY-13469 Debio 0932
Farnesyl Transferase FXR HY-104037 Cintirorgon HY-10912 Fexaramine
Fatty Acid Synthase (FAS) HCV Protease HY-101772 Ziritaxestat HY-14992 Bay 60-7550
Gutathione S-transferase HIV Integrase HY-18950 GSK2795039 HY-B0779 Teprenone
Nampt HIV Protease HY-15371 Forskolin HY-15768 Ilomastat
Pyruvate Kinase LXR HY-16278 Pradigastat HY-104042 Vorasidenib
Hydrolases: Mineralocorticoid Receptor HY-100218A RSL3 HY-15760 Necrostatin-1
Ester hydrolase Mitochondrial Metabolism HY-12270 T-5224 HY-109011 Rosiptor
Adenosine Deaminase RAR/RXR HY-B0763 Ibudilast HY-15148 Tipranavir
Aminopeptidase Reactive Oxygen Species HY-125840 PT2977 HY-13233A Talabostat
ACE ROR HY-100337 WWL70 HY-100742A (R)-GNE-140
Cathepsin Ser/Thr Protease HY-14896 Opicapone HY-100487 TAK-243
Dipeptidyl Peptidase HY-122218 JHU-083 HY-10231 PX-478
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Inhibitors • Agonists • Screening Libraries
Protein Tyrosine Kinase/RTK
Receptor Tyrosine Kinases Cat. No. Product Name Cat. No. Product Name
(RTKs): HY-16749 Pexidartinib (PLX-3397) HY-12050 CP-673451
ALK HY-112301 Pralsetinib (BLU-667) HY-12289 Defactinib (VS-6063)
c-Fms HY-P9907 Trastuzumab HY-18007 ALW-II-41-27
c-Kit HY-10997 Ibrutinib (PCI-32765) HY-100492 Fisogatinib (BLU-554)
c-Met/HGFR HY-114153 PLX5622 HY-101474A Zanubrutinib (BGB-3111)
Discoidin Domain Receptor HY-12768 BLZ945 HY-10181 Dasatinib (BMS-354825)
EGFR HY-109078 Vecabrutinib (SNS-062) HY-13342 Apatinib (YN968D1)
Ephrin Receptor HY-15150 Bemcentinib (R428; BGB324) HY-101916 Heparan
FGFR HY-16961 Sitravatinib (MGCD516) HY-129550 BI-4020
FLT3 HY-15772 Osimertinib (AZD-9291) HY-13024 Rebastinib (DCC-2036)
IGF-1R HY-P9905 Cetuximab (C225) HY-13016 Cabozantinib (XL184)
Insulin Receptor HY-P9906 Bevacizumab HY-10261 Afatinib (BIBW 2992)
PDGFR HY-10374 Semaxinib (SU5416) HY-15730 Poziotinib (HM781-36B)
RET HY-112306 Ripretinib (DCC-2618) HY-50895 Gefitinib (ZD1839)
ROS HY-10981 Lenvatinib (E7080) HY-10191 Linsitinib (OSI-906)
TAM Receptor HY-50904 Nintedanib (BIBF 1120) HY-13001 Quizartinib (AC220)
Trk Receptor HY-112299 TAS6417 HY-12823 BLU9931
VEGFR HY-109099 Pemigatinib (INCB054828) HY-101568 Roblitinib (FGF-401)
HY-18708 Erdafitinib (JNJ-42756493) HY-12866A Larotrectinib (LOXO-101)
HY-17600 Acalabrutinib (ACP-196) HY-112215 ARQ 531
Non-Receptor Tyrosine Kinases HY-P9912 Pertuzumab HY-13223 Crenolanib (CP-868596)
(NRTKs): HY-12432 Gilteritinib (ASP2215) HY-101549 MRX-2843 (UNC2371)
Ack1 HY-18750 AZD3759 HY-128757 Remibrutinib
Bcr-Abl HY-101977 Selitrectinib (LOXO-195) HY-15514A Merestinib (LY2801653)
BMX Kinase HY-100818 Futibatinib (TAS-120) HY-15458 SAR131675
Btk HY-13311 Infigratinib (BGJ-398) HY-15959 Savolitinib (Volitinib; AZD-6094)
FAK HY-114370 Selpercatinib (LOXO-292) HY-11092 BMS-509744
Itk HY-101561 Avapritinib (BLU-285) HY-109086 Edicotinib (JNJ-40346527)
Pyk2 HY-P0035 Insulin (human) HY-103022 Repotrectinib (TPX-0005)
Src HY-100342 Ibrutinib-biotin HY-10200 BMS-754807
Syk HY-104065 Pyrotinib (SHR-1258) HY-12857 Brigatinib (AP-26113)
HY-16069 Tucatinib (Irbinitinib; ONT-380) HY-50878 Crizotinib (PF-02341066)
HY-12215 Lorlatinib (PF-06463922) HY-19834 Fenebrutinib (GDC-0853)
HY-10331 Regorafenib (BAY 73-4506) HY-15764A A 419259 (RK 20449)
HY-100867A TAK-659 HY-101215 Evobrutinib (M2951)
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 MCE
Master of Small Molecules
Immunology/Inflammation
Aryl Hydrocarbon Receptor Cat. No. Product Name Cat. No. Product Name
CCR CD73 HY-12885B ADU-S100 (MIW815) HY-10218 Everolimus (RAD001)
Complement System HY-10037 Quiflapon (MK591) HY-15776 HG-9-91-01
COX CXCR HY-117287 BMS-986165 HY-101147 YKL-05-099
FKBP FLAP HY-11109 Resatorvid (TAK-242) HY-16046 Rimiducid (AP1903)
Galectin IFNAR HY-14882A Cenicriviroc (TAK-652) HY-17589 Chloroquine Phosphate
Interleukin Related HY-13756 Tacrolimus (FK506; Fujimycin) HY-B0579 Cyclosporin A (Cyclosporine)
IRAK MyD88 HY-12815A MCC950 (CP-456773; CRID3) HY-17627 Avacopan (CCX168)
NO Synthase HY-13992 AP20187 HY-108730 Avelumab
NOD-like Receptor (NLR) HY-P9904 Atezolizumab HY-102080 SAFit2
PD-1/PD-L1 PGE Synthase HY-18739 Phorbol 12-myristate 13-acetate HY-109044 Tapinarof (GSK2894512)
Reactive Oxygen Species HY-50937 ST 2825 HY-13740 Resiquimod (R848)
Salt-inducible Kinase (SIK) HY-112921B diABZI STING agonist-1 HY-109104 Telratolimod (MEDI 9197; 3M-052)
SPHK STING HY-10964 Vadimezan (DMXAA; ASA-404) HY-100116A Mitoquinone
Thrombopoietin Receptor HY-13245 PF-4136309 (INCB8761) HY-50674 INCB3344
Toll-like Receptor (TLR) HY-19745 BMS-202 HY-P9903 Nivolumab (BMS-936558)
Stem Cell/Wnt
Casein Kinase ERK Cat. No. Product Name Cat. No. Product Name
Gli GSK-3 HY-B0146 Verteporfin (CL 318952) HY-15147 XAV-939
Hedgehog Hippo (MST) HY-10182 CHIR-99021 (CT99021) HY-12681 CCT251545
JAK Notch HY-10071 Y-27632 HY-13418A Dorsomorphin (Compound C)
Oct3/4 PKA HY-16975 SH-4-54 HY-109049 Adavivint (SM04690)
Porcupine ROCK HY-50846 SCH772984 HY-19369 L-685458
sFRP-1 Smo HY-17545 LGK974 (WNT974) HY-116830 BRD0705
STAT TGF-beta/Smad HY-100526 XMU-MP-1 HY-13257 Thiazovivin
Wnt YAP HY-15307 SLx-2119 (KD-025) HY-11102 RO4929097 (RG-4733)
?-catenin ?-secretase HY-15392 Chroman 1 HY-14176 Compound E
HY-13027 DAPT (GSI-IX) HY-10590 TWS119
HY-14428 ICG-001 HY-16294 LY2090314
HY-50752 LY-411575 HY-14443 XMD8-92
HY-17024 Cyclopamine (11-Deoxojervine) HY-100830 NCB-0846
HY-15185 Nirogacestat (PF-3084014) HY-15659 Wnt-C59 (C59)
HY-13901 GANT 61 (NSC 136476) HY-10046 Plerixafor (AMD 3100)
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Inhibitors • Agonists • Screening Libraries
Anti-infection
Arenavirus Bacterial Cat. No. Product Name Cat. No. Product Name
CMV Enterovirus HY-104077 Remdesivir (GS-5734) HY-17362 Vancomycin
Filovirus Fungal HY-14882A Cenicriviroc (TAK-652) HY-B0490 Hygromycin B
HBV HCV HY-19930 Vaborbactam (RPX7009) HY-15148 Tipranavir (PNU-140690)
HIV HSV HY-109025 Baloxavir marboxil (S-033188) HY-13986 Merimepodib (VX-497)
Influenza Virus Parasite HY-12320 Cycloheximide (Actidione; CHX) HY-12983 ALS-8112
Reverse Transcriptase HY-17628 Cefiderocol (S-649266) HY-17409 Nystatin
RSV SARS-CoV HY-17565 Bleomycin HY-15303 Pritelivir (BAY 57-1293; AIC316)
Virus Protease HY-15695 Puromycin Aminonucleoside HY-10846 Delamanid (OPC-67683)
HY-18649 Galidesivir (BCX4430) HY-16727 Presatovir (GS-5806)
HY-50101A Mavorixafor (AMD-070 ) HY-10241 Simeprevir (TMC435)
HY-17006 Caspofungin Acetate (MK- 0991) HY-17586 Dalbavancin (BI-397)
HY-B1743A Puromycin (CL13900) HY-15597 Salinomycin (Procoxacin)
HY-17589 Chloroquine HY-14989 SQ109 (NSC722041)
HY-A0098 Tunicamycin HY-13004 Maraviroc (UK-427857)
HY-12594 Paritaprevir (ABT-450) HY-14768 Favipiravir (T-705)
HY-14865C Omadacycline (PTK0796) HY-13238 Dolutegravir (S/GSK1349572)
HY-N0565B Doxycycline HY-112205A RR-11a analog
HY-14434 Asunaprevir (BMS-650032) HY-10493 Cobicistat (GS-9350)
HY-12559 Alisporivir (Debio-025) HY-B0117 Tigecycline (GAR-936)
HY-P0025 NIM811 HY-101954 Inarigivir
HY-13740 Resiquimod (R848) HY-16468 Squalamine (MSI-1256)
HY-16742 Gepotidacin (GSK2140944) HY-15460 CHIR-090
HY-100029 Bay 41-4109 HY-90001 Ritonavir (ABT 538)
HY-14879A Avibactam (NXL-104) HY-15233 Letermovir (AIC246)
HY-104012 Islatravir (MK-8591) HY-B0522A Ampicillin
HY-13318 Oseltamivir acid (GS 4071) HY-16973 Fluralaner (A1443)
HY-14737 Ceftaroline fosamil (TAK-599) HY-101479 Iclaprim (AR-100)
HY-17367A Atazanavir (BMS-232632) HY-10373 Trimetrexate (CI-898)
HY-17605 Bictegravir (GS-9883) HY-B1123 Auranofin (SKF-39162)
HY-15287A Nelfinavir (AG-1343) HY-16980A Eravacycline (TP-434)
HY-17561 G-418 (Geneticin) HY-15298 Grazoprevir (MK-5172)
HY-16752 Relebactam (MK-7655) HY-135747 Gut restricted-7
HY-112579 Ceftobiprole (Ro 63-9141) HY-P0017 Aprotinin
HY-14881 Bedaquiline (TMC207) HY-10392 Sutezolid (PNU-100480)
HY-16730 Sarolaner (PF-6450567) HY-17593 Solithromycin (CEM-101)
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Master of Small Molecules
JAK/STAT Signaling
EGFR JAK Cat. No. Product Name Cat. No. Product Name
Pim STAT HY-19322B PIM-447 (LGH447) HY-104065 Pyrotinib (SHR-1258)
HY-117287 BMS-986165 HY-16069 Tucatinib (Irbinitinib)
HY-P9907 Trastuzumab HY-129550 BI-4020
HY-109053 Delgocitinib (JTE-052) HY-10261 Afatinib (BIBW 2992)
HY-19569 Upadacitinib (ABT-494) HY-15730 Poziotinib (HM781-36B)
HY-15772 Osimertinib (AZD-9291) HY-50895 Gefitinib (ZD1839)
HY-P9905 Cetuximab (C225) HY-100754 PF-06651600
HY-50856 Ruxolitinib (INCB18424) HY-10409 Fedratinib (TG-101348)
HY-16975 SH-4-54 HY-16997 Itacitinib (INCB039110)
HY-112299 TAS6417 HY-50896 Erlotinib (CP-358774)
HY-P9912 Pertuzumab HY-15146 NSC 74859 (S3I-201)
HY-18750 AZD3759 HY-100494 SH5-07
HY-104065B Pyrotinib (SHR-1258) HY-13050 Sapitinib (AZD-8931)
HY-40354 Tofacitinib (CP-690550) HY-16379 Pacritinib (SB1518)
HY-18960 CHZ868 HY-111553 TAS0728
MAPK/ERK Pathway
ERK Cat. No. Product Name Cat. No. Product Name
JNK HY-15605 Encorafenib (LGX818) HY-18972 PLX8394
KLF HY-50846 SCH772984 HY-50706 Selumetinib (AZD6244)
MAP3K HY-10256 SB 203580 HY-10999A Trametinib (GSK-1120212)
MAP4K HY-100022 Tomivosertib (eFT508) HY-14660 Dabrafenib (GSK2118436)
MAPKAPK2 (MK2) HY-12057 Vemurafenib (PLX4032) HY-10254 PD0325901
MEK HY-18938 Selonsertib (GS-4997) HY-10402 Losmapimod (GW856553X)
Mixed Lineage Kinase HY-12028 PD98059 HY-15202 Binimetinib (MEK162)
MNK HY-12031 U0126 HY-12599 URMC-099
p38 MAPK HY-13064 Cobimetinib (GDC-0973) HY-12558 LY3009120 (DP-4978)
Raf HY-10201 Sorafenib (Bay 43-9006) HY-10295 SB 202190
Ribosomal S6 Kinase (RSK) HY-32018 Cot inhibitor-2 HY-12947 GNE-3511
HY-15947 Ravoxertinib (GDC-0994) HY-15816 Ulixertinib (BVD-523)
HY-112082 BAY885 HY-103490 Takinib
HY-10999 Trametinib (GSK1120212) HY-52101 CMK
HY-112089 LXH254 HY-10510 BI-D1870
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Inhibitors • Agonists • Screening Libraries
GPCR/G Protein
Class A: Kisspeptin Receptor Cat. No. Product Name Cat. No. Product Name
Adenosine Receptor Leukotriene Receptor HY-114277 AMG-510 HY-15778 AVE 0991
Adenylate Cyclase LPL Receptor HY-U00418 ARS-1620 HY-15418 RS 504393
Adiponectin Receptor mAChR HY-15677 INT-777 HY-19870 Setmelanotide
Adrenergic Receptor MCHR1 (GPR24) HY-130149 MRTX849 HY-13951 ICI 118,551
Adrenergic Receptor Melanocortin Receptor HY-112185 GLP-1 receptor agonist 1 HY-12355 Siponimod
Angiotensin Receptor Melatonin Receptor HY-12434 INT-767 HY-15848 AdipoRon
Apelin Receptor mGluR HY-13948 Angiotensin II human HY-10017 SCH 546738
Bombesin Receptor Motilin Receptor HY-P0014 Liraglutide HY-P0202 Endothelin 1
Bradykinin Receptor Neurokinin Receptor HY-13245 PF-4136309 HY-101952 Prostaglandin E2
Cannabinoid Receptor Neuromedin U receptor 2 HY-32709 Telcagepant HY-100619 BMS-986020
CaSR Neuropeptide Y Receptor HY-15608 MPTP HY-10198 Navarixin
CCR Neurotensin Receptor HY-50101A Mavorixafor HY-114118A Semaglutide
CGRP Receptor Opioid Receptor HY-15403A Atrasentan HY-111343 ONC212
Cholecystokinin Receptor Orexin (OX) Receptor HY-15252 Reparixin HY-10302 MK-3207
Class A Orphans Oxytocin Receptor HY-13443 Exendin-4 HY-10480 Fasiglifam
CRFR P2Y Receptor HY-101978 CPI-444 HY-B0606 Diquafosol
CXCR Platelet-Activating Factor HY-126247 BI-2852 HY-14870 Selexipag
Dopamine Receptor Receptor HY-114436 MRTX-1257 HY-P0171 Motixafortide
EBI2/GPR183 Prolactin-Releasing Peptide HY-13848 AZD8797 HY-14779 Riociguat
Endothelin Receptor Receptor HY-103088 E7046 HY-B0879A Suramin
Formylpeptide Receptor Prostaglandin Receptor HY-14864 Mapracorat HY-114398 BAY-293
GHSR Protease-Activated HY-15894 BQ-788 HY-A0013 Bosentan
Glucocorticoid Receptor Receptor (PAR) HY-19855 AZD-5069 HY-N0583 Hydrocortisone
GNRH Receptor Ras HY-119243 LY2794193 HY-P0082 Glucagon
GPCR19 RGS Protein HY-15319 AMG 487 HY-100775 Setogepram
GPR109A Sigma Receptor HY-50674 INCB3344 HY-10013 Taranabant
GPR119 Somatostatin Receptor HY-12802 AF38469 HY-12080 BX471
GPR120 TSH Receptor HY-101295 Pan-RAS-IN-1 HY-112558 AZ3451
GPR139 Urotensin Receptor HY-19706 ARS-853 HY-16774 Vericiguat
GPR40 Vasopressin Receptor HY-14648 Dexamethasone HY-103193 NKH477
GPR55 Class B: HY-10095 Olcegepant HY-17000 Tolvaptan
GPR84 Glucagon Receptor HY-101980 AZD4635 HY-19904 Adomeglivant
Guanylate Cyclase VIP and PACAP Receptors HY-16168A Degarelix HY-12378 BQ-123
Histamine Receptor HY-P0264 Avexitide HY-B0075 Melatonin
Imidazoline Receptor HY-108677 L-368,899 HY-U00416 ARS-1323
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 MCE
Master of Small Molecules
Neuronal Signaling
5-HT Receptor AChE Cat. No. Product Name Cat. No. Product Name
Adenosine Kinase HY-17366 Clozapine (N-oxide) HY-15084 Dizocilpine (MK-801)
Adrenergic Receptor HY-A0190 Ceruletide (Caerulein) HY-10448 Capsaicin
Amyloid-? Beta-secretase HY-15424 5-Iodotubercidin (NSC 113939) HY-112723 ACT-709478
Calcium Channel HY-32709 Telcagepant (MK-0974) HY-12449 Crenigacestat (LY3039478)
CaMK HY-15608 MPTP HY-15064 HC-030031
Cannabinoid Receptor HY-107422 PAT-1251 HY-12650 Mirogabalin (DS5565)
CGRP Receptor HY-42110 Deschloroclozapine HY-101386 PZM21
Cholecystokinin Receptor HY-14896 Opicapone (BIA 9-1067) HY-18779 PF-4840154
COMT HY-100740 Lanabecestat (AZD3293) HY-10809 Bitopertin (RG1678)
Dopamine Receptor HY-15498 Rimegepant (BMS-927711) HY-B0468 Isoprenaline (Isoproterenol)
Dopamine Transporter HY-12802 AF38469 HY-14773 Mirabegron (YM178)
FAAH GABA Receptor HY-19608 GSK1016790A HY-16567 Asenapine
GlyT GPR119 HY-10095 Olcegepant (BIBN-4096) HY-P0183 Nociceptin (Orphanin FQ)
GPR139 GPR55 HY-50752 LY-411575 HY-P1061A Colivelin
Histamine Receptor HY-19733 Lumateperone (ITI-007) HY-14557A Pimavanserin (ACP-103)
iGluR HY-103040 Zuranolone HY-19654 GSK598809
Imidazoline Receptor HY-P1363 Amyloid ?-Peptide (1-42) HY-106224 Orexin A
mAChR HY-50682 Azeliragon (TTP488) HY-10341 Fasudil (HA-1077)
MCHR1 (GPR24) HY-101736 AMG9810 HY-13526 YO-01027 (Dibenzazepine; DBZ)
Melanocortin Receptor HY-P0128 Amyloid beta-peptide(25-35) HY-12777 Asivatrep (PAC-14028)
Melatonin Receptor HY-10302 MK-3207 HY-15296 Cabergoline (FCE-21336)
mGluR HY-15068 NBQX (FG9202) HY-19370 FPS-ZM1
Monoamine Oxidase HY-12428 A-1165442 HY-13410 Xanomeline (LY246708)
nAChR HY-101507 Pico145 (HC-608) HY-16725 Lemborexant (E-2006)
Neurokinin Receptor HY-19369 L-685458 HY-12882A Ifenprodil
Neuropeptide Y Receptor HY-N2332A Methyllycaconitine citrate HY-19545A SCH 23390
Neurotensin Receptor HY-108337 GNE 0723 HY-15370A SB-269970
Notch HY-B0102A Fluoxetine (LY-110140) HY-P0117 Tat-NR2B9c (NA-1)
Opioid Receptor HY-100714A D-AP5 HY-101299B Dihydrexidine (DAR-0100)
Orexin Receptor (OX Receptor) HY-14176 Compound E HY-P0201 Substance P
Serotonin Transporter HY-B0075 Melatonin HY-17631A Edonerpic (T-817MA)
Sigma Receptor HY-B0726 Pilocarpine HY-14763A Cariprazine (RGH188)
Somatostatin Receptor HY-14280 Entacapone HY-13438 AZD3839
Trk Receptor TRP Channel HY-12745A Nalfurafine (TRK-820) HY-70059 LY341495
?-secretase HY-108690 Fluxametamide HY-16579A Etifoxine
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 www.MedChemExpress.com
Inhibitors • Agonists • Screening Libraries
Membrane Transporter/Ion Channel
ATP Synthase Cat. No. Product Name Cat. No. Product Name
BCRP HY-12750 AZD3965 HY-108337 GNE 0723
Calcium Channel HY-15763 Erastin HY-19778 (R)-BPO-27
CFTR HY-100558 Bafilomycin A1 HY-15699 SAR7334
Chloride Channel HY-100720 GSK2193874 HY-N2143 Fumitremorgin C
CRAC Channel HY-15598 20-HETE HY-112302 HC-070
CRM1 HY-17607 Cenobamate (YKP3089) HY-13017 Ivacaftor (VX-770)
EAAT2 HY-10010 Ko 143 HY-100714A D-AP5
GABA Receptor HY-15409 Empagliflozin (BI 10773) HY-12693 R(+)-IAA-94
GlyT HY-50879 Elacridar (GF120918) HY-101455 CDN1163
HCN Channel HY-111772 Elexacaftor (VX-445) HY-15084 Dizocilpine (MK-801)
iGluR HY-50694 Senicapoc (ICA-17043) HY-10448 Capsaicin
Monoamine Transporter HY-15718A Istaroxime (PST2744) HY-112723 ACT-709478
Monocarboxylate Transporter HY-13248 AR-C155858 HY-12343 ML277 (CID-53347902)
Na+/Ca2+ Exchanger HY-19608 GSK1016790A HY-100965 Diphenyleneiodonium chloride (DPI)
Na+/HCO3- Cotransporter HY-100381 Nigericin HY-15064 HC-030031
Na+/K+ ATPase HY-13433 Thapsigargin HY-12650 Mirogabalin (DS5565)
nAChR HY-100390 (S)-ML753286 HY-50671 Zosuquidar (LY-335979)
NKCC HY-10450 Dapagliflozin (BMS-512148) HY-101840 EIPA (L593754)
P-glycoprotein HY-103040 Zuranolone HY-101664 Ilaprazole (IY-81149)
P2X Receptor HY-15553A Mibefradil (Ro 40-5967) HY-18779 PF-4840154
Potassium Channel HY-101588 Gefapixant (MK-7264) HY-10809 Bitopertin (RG1678)
Proton Pump HY-101736 AMG9810 HY-111651 Gboxin
SGLT HY-10451 Canagliflozin (JNJ 28431754) HY-16738A Eleclazine (GS 6615)
Sodium Channel HY-13434 Ionomycin HY-17384 Valspodar (PSC 833)
TRP Channel HY-101942 CM-4620 HY-12777 Asivatrep (PAC-14028)
URAT1 HY-15068 NBQX (FG9202) HY-12758A YHO-13351
VDAC HY-15640 Capsazepine HY-15258 Lesinurad (RDEA594)
HY-15991 Tenapanor (AZD1722) HY-12882A Ifenprodil
HY-12428 A-1165442 HY-100208 HC-067047
HY-101507 Pico145 (HC-608) HY-14483 AF-353 (Ro-4)
HY-111925 BI-749327 HY-P0117 Tat-NR2B9c (NA-1)
HY-13519 TRAM-34 HY-10634 AMG 517
HY-16589 Oligomycin A (MCH 32) HY-13646 Encequidar (HM30181)
HY-N2332A Methyllycaconitine HY-111325 Synta66
HY-12883 PF 05089771 HY-B1140 Diazoxide (Sch-6783)
11

 MCE
Master of Small Molecules
Cytoskeleton
Arp2/3 Complex Cat. No. Product Name Cat. No. Product Name
Dynamin HY-13442A Eribulin Mesylate HY-19792 Mertansine (DM1)
Gap Junction Protein HY-15575 VcMMAE HY-13441 (-)-Blebbistatin
Integrin HY-15162 Monomethyl auristatin E (MMAE) HY-10913A Danegaptide (GAP-134)
Kinesin HY-15584 Taltobulin (HTI-286; SPA-110) HY-16141 Cilengitide (EMD 121974)
Microtubule/Tubulin HY-10222 Ixabepilone (BMS 247550) HY-14951 Firategrast (SB 683699)
Mps1 HY-15578 McMMAF HY-18676 OSU-T315
Myosin HY-B0015 Paclitaxel (Taxol) HY-15102 MK-0429 (L-000845704)
PAK HY-106268A Larazotide HY-N0488 Vincristine (Leurocristine)
HY-15583 Auristatin F HY-50759 Ispinesib (SB-715992)
HY-15204 Tonabersat (SB-220453) HY-12454 DM4
HY-B0011 Docetaxel (RP-56976) HY-P0023 Cyclo(-RGDfK)
HY-15278 Epothilone D (KOS 862) HY-12793 KPT-9274
HY-15886 Mdivi-1 HY-P0122 iRGD peptide (c(CRGDKGPDC))
HY-17029 Epothilone B (Patupilone) HY-13007 PF-3758309
HY-112162 BOS-172722 HY-12858 Empesertib (BAY 1161909)
NF-?B
IKK Cat. No. Product Name Cat. No. Product Name
Keap1-Nrf2 HY-112433 NIK SMI1 HY-112675 4-Octyl Itaconate
MALT1 HY-12212 Omaveloxolone (RTA-408) HY-P0151 SN50
NF-?B HY-18950 GSK2795039 HY-16561 Resveratrol (SRT501)
Reactive Oxygen Species HY-100523 ML385 HY-13060 ACHP (IKK-2 Inhibitor VIII)
HY-15473 MLN120B HY-B0215 Acetylcysteine (NAC)
HY-12213 CDDO-EA (RTA 405) HY-111941 GSK8612
HY-19356 Rocaglamide (Roc-A) HY-12276 MALT1 inhibitor MI-2
HY-100116A Mitoquinone (MitoQ) HY-18935A CBL0137
HY-101140 KI696 HY-115466 MLT-748
HY-13324 Bardoxolone (RTA 402) HY-B1960 Canthaxanthin
HY-13755 Sulforaphane HY-N0005 Curcumin
HY-D0937 Methoxy-PMS HY-13019 BI605906
HY-13453 BAY 11-7082 (BAY 11-7821) HY-14645 (-)-DHMEQ
HY-15725 CDDO-Im (RTA-403; TP-235) HY-13982 JSH-23
HY-D0940 H2DCFDA HY-10514 BX795
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 www.MedChemExpress.com
Inhibitors • Agonists • Screening Libraries
TGF-beta/Smad
PKC Cat. No. Product Name Cat. No. Product Name
ROCK HY-10230 Midostaurin (PKC412) HY-13434 Ionomycin (SQ23377)
TGF-beta/Smad HY-13226 Galunisertib (LY2157299) HY-10343 Sotrastaurin (AEB071)
TGF-? Receptor HY-10431 SB-431542 HY-13012 RepSox (E-616452)
HY-10071 Y-27632 HY-103021 LY3200882
HY-15141 Staurosporine HY-N0439 Asiaticoside
HY-12043 SB 525334 HY-12953 R-268712
HY-15307 SLx-2119 (KD-025) HY-P0118 Disitertide (P144)
HY-15392 Chroman 1 HY-10195B Ruboxistaurin (LY 333531)
HY-12075 LY2109761 HY-15685 Ripasudil (K-115)
HY-13013 (E)-SIS3 HY-13689 Go 6983 (Gö 6983)
HY-B0673 Pirfenidone (AMR69) HY-12659 LX7101
HY-100347A SRI-011381 HY-13521 SB-505124
HY-19928 Vactosertib (TEW-7197) HY-13867 Bisindolylmaleimide I
HY-10432 A 83-01 HY-10342 Enzastaurin (LY317615)
HY-12071 LDN193189 (DM-3189) HY-112782 VTX-27
Vitamin D Related
Vitamin D Cat. No. Product Name
Vitamin D Receptor (VDR) HY-10002 Calcitriol (1,25-Dihydroxyvitamin D3)
HY-A0020 Eldecalcitol (ED-71; 2-(3-hydroxypropoxy)-1,25-dihydroxyvitamin D3)
HY-32343 Secalciferol ((24R)-24,25-Dihydroxyvitamin D3)
HY-15830 25,26-Dihydroxyvitamin D3 (25,26-Dihydroxycholecalciferol)
HY-10001 Calcipotriol (MC 903; Calcipotriene)
HY-50919 Paricalcitol
HY-76915 24, 25-Dihydroxy VD3
HY-77274 Calcitriol Impurities D
HY-15254 3-O-(2-Aminoethyl)-25-hydroxyvitamin D3
HY-76801 24, 25-Dihydroxy VD2 (24,25-Dihydroxy vitamin D2)
HY-32350 Ercalcitriol (1?,25-Dihydroxy Vitamin D2)
HY-32342 Falecalcitriol
HY-15332 Alfacalcidol-D6
HY-32349 Ercalcidiol (25-hydroxy Vitamin D2)
HY-15157 Calcitetrol (1?, 24, 25-Trihydroxy VD3)
13

 MCE
Master of Small Molecules
Antibody-drug Conjugate/ADC Related
The antibody-drug conjugate (ADC) is a humanized or human monoclonal antibody conjugated with highly cytotoxic small molecules
(payloads) through chemical linkers. ADCs increase the cell-killing potential of monoclonal antibodies (mAbs), and confer higher tumor selectivity.
Some ADCs has been approved by FDA.
ADC Cytotoxin
Destroys cancer cells
50+
ADC Cytotoxins
Cat. No. Product Name
HY-15162 Monomethyl auristatin E ADC Linker
Joins antibody and drug
HY-15162A D8-MMAE
HY-15584 Taltobulin
HY-15142 Doxorubicin Hydrochloride
HY-13316 Mitomycin C Antibody
Targets cancer cells
HY-19610 alpha-Amanitin
HY-B0015 Paclitaxel
HY-15583 Auristatin F Drug-Linker Conjugates for 500+
HY-16261 Aldoxorubicin ADC ADC Linkers
HY-19609 Calicheamicin Cat. No. Product Name Cat. No. Product Name
HY-19792 Mertansine HY-15575 VcMMAE HY-78738 MC-Val-Cit-PAB
HY-13631D Dxd HY-15578 McMMAF HY-12362 Val-cit-PAB-OH
HY-13062 Daunorubicin Hydrochloride HY-101070 SMCC-DM1 HY-41189 Fmoc-Val-Cit-PAB-PNP
HY-14519 Methotrexate HY-13631E Deruxtecan HY-20336 Mc-Val-Cit-PABC-PNP
HY-13704 SN-38 HY-100374 Val-Cit-PAB-MMAE HY-43869 Vipivotide tetraxetan Linker
HY-15579A MMAF Hydrochloride HY-111012 DBCO-(PEG)3-VC-PAB-MMAE HY-42973 DBCO-NHS ester
HY-16700 PNU-159682 HY-100566 SuO-Val-Cit-PAB-MMAE HY-114430 Fmoc-Phe-Lys(Boc)-PAB-PNP
HY-13061 Daun02 HY-117410 Vipivotide tetraxetan HY-100216 SPDP
HY-15579AS D8-MMAF Hydrochloride HY-126681 SC-VC-PAB-MMAE HY-19318 Fmoc-Val-Cit-PAB
HY-16560 Camptothecin