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Histone Methyltransferase

Histone Methyltransferase

Histone modifications are essential for controlling both overall gene expression and stage-specific gene expression. While histones H3K9 and H3K27 are typically associated with gene repression, methylation on histones H3K4, H3K36, and H3K79 is typically associated with gene activation. Site-specific methyltransferases and demethylases dynamically control the methylation of histone lysines. The methylation of H3K27 in cells is carried out by EZH2 (the catalytic subunit of PRC2).
Inhibiting DOT1L, a histone H3 lysine 79 methyltransferase, improves the production of induced pluripotent stem cells (iPSCs). A powerful and specific DOT1L inhibitor, EPZ-5676.

The histone methyltransferase enhancer of zeste homolog 2 (EZH2) trimethylates histone 3's lysine 27 (H3K27me3), which results in chromatin condensation and transcriptional repression and is essential for PRC2 activity.

Histone Methyltransferase related products

Structure Cat No. Product Name CAS No. Product Description
(R)-AMG-193 V103416 (R)-AMG-193 2790567-83-6 (R)-AMG-193 is an isomer of AMG 193.
3-去氮腺嘌呤A V0384 3-deazaneplanocin A (DZNeP; NSC 617989) HCl 120964-45-6 3-deazaneplanocin A HCl (known also asDZNep; C-c3Ado; NSC-617989), the hydrochloride salt of 3-deazaneplanocin A which is an adenosineanalog, is a novel and competitive inhibitor of S-adenosylhomocysteine hydrolase and also an EZH2(histone methyltransferase) inhibitor with anticancer activity.
5WKS V2032 5WKS 1350752-07-6 G9a-IN-1 (Compound 113) is a G9a protein inhibitor.
[Nle20] H4 peptide (16−23) V101211 [Nle20] H4 peptide (16−23) 2042178-19-6 [Nle20] H4 peptide (16−23) is a peptide with strong inhibitory activity against histone methyltransferase SETD8 (Kd=0.14μM). It inhibits SETD8 methylation of histone H4 by competing for the substrate binding site of SETD8.
A-196 V3067 A-196 1982372-88-2 A-196 (A196) is a potent, selective and first-in-class inhibitor of SUV420H1 and SUV420H2 (IC50= 25 and 144 nM) with anticancer activity.
A-366 V9842 A-366 1527503-11-2 A-366 (A366) is a novel, potent and peptide-competitive inhibitor of thehistone methyltransferase G9a with anticancer activity.
AC1Q3QWB (AQB) V85805 AC1Q3QWB (AQB) 46697-00-1
AMG-193 V75868 PRMT5-IN-27 2790567-82-5 PRMT5-IN-27 (compound 481) is an inhibitor (blocker/antagonist) of PRMT5.
AMI-408 V98450 AMI-408 78866-14-5 AMI-408 is a PRMT1 inhibitor.
Amodiaquine-d10 V56266 Amodiaquine-d10 1189449-70-4 Amodiaquine-d10 is the deuterium labelled form of Amodiaquine.
Anticancer agent 126 V78961 Anticancer agent 126 Anticancer agent 126 (compound 12) is a WDR5 inhibitor (antagonist) with anticancer effects.
Antiproliferative agent-25 V79864 Antiproliferative agent-25 antiproliferation agent-25 (Compound 3s4) is a selective PRMT5 inhibitor (IC50= 0.11 μM).
Antitumor agent-101 V34821 Antitumor agent-101 2848632-52-8 Antitumor agent-101 is a selective covalent inhibitor of lysine methyltransferase G9a/GLP, with IC50s of 8.5 nM and 5.5 nM for G9a and GLP, respectively.
AS-254s V105086 AS-254s AS-254s is an inhibitor of deleted, small, or homologous-like 1 protein (ASH1L) with IC50 of 94 nM (FP assay).
AS-85 V52392 AS-85 2323623-80-7 AS-85 is a potent ASH1L inhibitor (IC50=0.6 µM) with anti-leukemia activity.
AS-99 V78137 AS-99 AS-99 is a first-in-class, potent and specific ASH1L histone methyltransferase inhibitor (IC50= 0.79 µM, Kd= 0.89 µM) and has anti-leukemia activity.
AS-99 TFA V77240 AS-99 TFA AS-99 TFA is a first-in-class, potent and specific ASH1L histone methyltransferase inhibitor (IC50= 0.79 µM, Kd= 0.89 µM) with anti-leukemia activity.
AZ-505 2TFA salt V12013 AZ-505 2TFA salt 1035227-44-1 AZ-505(AZ505) 2TFA, the ditrifluoroacetate salt ofAZ-505, is an SMYD2 (SET and MYND domain-containing protein 2)inhibitor with anticancer activity.
AZ-PRMT5i-1 V99818 AZ-PRMT5i-1 2918814-96-5 AZ-PRMT5i-1 (Compound 28) is a potent, oral MTAP-selective PRMT5 inhibitor.
AZ506 V52369 AZ506 2043321-54-4 AZ506 is a potent SMYD2 inhibitor (antagonist) with IC50 of 17 nM.
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