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Epigenetics
Product Handbook
MCE
Master of Bioactive Molecules
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.
1
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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.
2
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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.
3
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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.
4
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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].
5
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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
6
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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].
7
MCE
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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.
8
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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
9
MCE
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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Epigenetics
Product Handbook
MCE
Master of Bioactive Molecules
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
www.MedChemExpress.com
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.
1
MCE
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.
2
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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.
3
MCE
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.
4
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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].
5
MCE
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
6
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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].
7
MCE
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.
8
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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
9
MCE
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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jeudi 23 mai 2024