Histone Methyltransferase

Angiogenesis

5-alpha Reductase ALK Bcr-Abl BTK EGFR FAK FLT3 HER-2 HIF Src Syk VDA VEGFR
Anti-infection

Antibiotic Arenavirus Bacterial CMV EBV Enterovirus Filovirus Fungal Gli HBV HCV HCV Protease HIV HSV Influenza Virus Parasite RABV Reverse Transcriptase RSV SARS-CoV TMV Virus Protease
Apoptosis

Apoptosis ASK Bcl-2 Caspase c-Myc c-RET Cytohesin DAPK Ferroptosis FKBP IAP Mdm2 p53 PD-1 PD-L1 PERK PKD Ras RIP kinase ROS Survivin Thymidylate Synthase TNF Receptor TNFa TRADD
Autophagy

Autophagy LRRK2 Mitophagy OGA ULK
Cell Cycle

Antifolate APC Aurora Kinase BMI-1 CDK Chk c-Myc Eukaryotic Initiation Factor G-quadruplex HDAC HSP Kinesin LIMK Mad2 Microtubule(Tubulin) Mps1 Nucleoside Antimetabolite/Analog Nur77 p21 PAK PERK PFKFB PLK PPAR Ras Rho ROCK SRPK TOPK Topoisomerase Wee1
Cytoskeletal Signaling

Arp2 3 Complex Bcr-Abl Cardiac Myosin Dynamin Gap Junction Protein HSP Integrin Kinesin Microtubule Associated MLCK Myosin PAK TACC3 Wntbeta-catenin
DNA Damage

ATM(ATR) CRISPR(Cas9) DNA alkylator DNA Stain DNA(RNA) Synthesis GAK HDAC HSP Nucleoside Antimetabolite(Analog) OGG1 p97 PARG PARP RAD51 RNR Sirtuin SMN Telomerase Topoisomerase
Endocrinology & Hormones

5-alpha Reductase ACE Adrenergic Receptor Androgen Receptor Aromatase Estrogenprogestogen Receptor Glucocorticoid Receptor GPR Mineralocorticoid Receptor RAAS THR TSH Receptor
Epigenetics

AMPK Aurora Kinase DNA Methyltransferase Epigenetic Reader Domain EZH1 2 HDAC HIF Histone Acetyltransferase Histone Demethylase Histone Methyltransferase JAK MAT MicroRNA MLL Pim PKC Protein Arginine Deiminase Sirtuin Small Interfering RNA (siRNA) SMYD
GPCR & G Protein

5-HT Receptor Adenosine Receptor Adenylate Cyclase Adrenergic Receptor Angiotensin Receptor APJ Bombesin Receptor Bradykinin Receptor cAMP Cannabinoid Receptor CaSR CCK receptor CCR CGRP Receptor CRFR CXCR Dopamine Receptor EBI2 Endothelin Receptor Formyl Peptide Receptor Free Fatty Acid Receptor G protein-coupled Bile Acid Receptor GCGR GHSR GLP Receptor Glucagon Receptor GnRH Receptor GPCR19 GPR GPR109A Guanylate Cyclase Hedgehog(Smoothened) ROCK Histamine Receptor ICMT Leukotriene Receptor LPA Receptor LPL Receptor LTR mAChR Melanocortin Receptor Melatonin Receptor mGluR Motilin Receptor MRGPR MT Receptor Neurokinin Receptor Neuropeptide Y Receptor Neurotensin Receptor NPY receptor Opioid Receptor OX Receptor Oxytocin Receptor P2Y Receptor PAFR PAR PKD PKG Prostaglandin Receptor Ras RGS Protein S1P Receptor SGLT Sigma Receptor Somatostatin Receptor TAAR TSH Receptor Urotensin Receptor Vasopressin Receptor

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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

Cat No.	Product Name	CAS No.	Product Description
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.
V2032	5WKS	1350752-07-6	G9a-IN-1 (Compound 113) is a G9a protein inhibitor.
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.
V9842	A-366	1527503-11-2	A-366 (A366) is a novel, potent and peptide-competitive inhibitor of thehistone methyltransferase G9a with anticancer activity.
V0388	AMI-1 disodium salt	20324-87-2	AMI-1 (AMI 1) disodium saltis a novel, cell-permeable and selective inhibitor of Histone Methyltransferase (HMT) with anti-inflammatory activity.
V6409	Amodiaquin HCl hydrate	6398-98-7	Amodiaquin dihydrochloride(trade names Camoquin, Flavoquine)isa potent and orally bioactive inhibitor of the Ebola virus, acts by targeting the viral protein 35 (VP35).
V56266	Amodiaquine-d10	1189449-70-4	Amodiaquine-d10 is the deuterium labelled form of Amodiaquine.
V78961	Anticancer agent 126		Anticancer agent 126 (compound 12) is a WDR5 inhibitor (antagonist) with anticancer effects.
V79864	Antiproliferative agent-25		antiproliferation agent-25 (Compound 3s4) is a selective PRMT5 inhibitor (IC50= 0.11 μM).
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.
V52392	AS-85	2323623-80-7	AS-85 is a potent ASH1L inhibitor (IC50=0.6 µM) with anti-leukemia activity.
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.
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.
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.
V52369	AZ506	2043321-54-4	AZ506 is a potent SMYD2 inhibitor (antagonist) with IC50 of 17 nM.
V4167	BAY-598	1906919-67-2	BAY-598 (BAY598 S-isomer) is novel, potent, selective and peptide-competitive small molecule inhibitor of lysine methyltransferaseSMYD2 with potential antitumor activity.
V52360	BBDDL2059	2691174-27-1	BBDDL2059 is a selective covalent inhibitor of the histone methyltransferase EZH2 with IC50 of 1.5 nM for EZH2-Y641F.
V6240	BCI-121	432529-82-3	BCI-121 is a SMYD3 inhibitor that can suppress cancer/tumor cell growth/proliferation.
V0381	BIX 01294	935693-62-2	BIX01294 is a novel and potent inhibitor of G9a histone methyltransferase with anticancer activity.
V3451	BIX01294 triHCl	1392399-03-9	BIX01294 triHCl (the tri-hydrochloride salt of BIX01294) is a novel and potent inhibitor of G9a histone methyltransferase with IC50 of 2.7 μM in a cell-free assay.