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

+MORE

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
V76745	MRTX-1719 hydrochloride		MRTX-1719 HCl is a potent, first-in-class, selective inhibitor of the PRMT5/MTA complex, with IC50 of <10 nM for the PRMT5/MTA MTAPDEL SDMA cell line.
V76744	MRTX9768 hydrochloride		MRTX9768 HCl is a potent, selective, orally bioactive, first-in-class inhibitor of the PRMT5-MTA complex.
V51600	MS-023 trihydrochloride	2108631-19-0	MS023 triHClide is a potent, cellularly active inhibitor of human type I protein arginine methyltransferases (PRMTs), with IC50s of 30, 119, 83, and 4 for PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8, respectively.
V51744	MS-33	2407449-11-8	MS33 is a potent WDR5 degrader with Kds of 870 nM and 120 nM for VCB and WDR5, respectively.
V51748	MS-67	2407452-77-9	MS67 is a potent and specific WD40 repeat domain protein 5 (WDR5) degrader with Kd of 63 nM.
V3032	MS023	1831110-54-3	MS023 (MS-023) is a novel, potent, selective, and cell-active inhibitor of PRMTs (Protein arginine methyltransferases) with potential anticancer activity.
V31954	MS023 dihydrochloride	1992047-64-9	MS023 diHCl is a potent, selective, and cellularly active inhibitor of human type I protein arginine methyltransferases (PRMTs), with IC50s of 30, 119, and 83 for PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8, respectively.
V38885	MS049	1502816-23-0	MS049 (MS 049; MS-049) is a potent and selective inhibitor of protein arginine methyltransferases-PRMT4 and PRMT6 with potential antineoplastic activity.
V2604	MS049 2HCl	2095432-59-8	MS049 (MS-049; MS 049) 2HCl,the dihydrochloride salt of MS-049, is a potent and selective PRMT4 and PRMT6 inhibitor with potential anticancer activity.
V75875	MS117	2702280-86-0	MS117 is a first-in-class, cell-active, irreversible/covalent inhibitor of protein arginine methyltransferase (PRMT6) with IC50 of 18 nM.
V40191	MS1943	2225938-17-8	MS1943 (MS-1943) is a novel and potent EZH2 degrader(IC50 = 120 nM) with anticancer activity.
V75874	MS8511	2866408-21-9	MS8511 is a selective, covalent, irreversible inhibitor of G9a/GLP that targets cysteine residues in the substrate binding site, with IC50s of 100 nM (G9a) and 140 nM (GLP), and Kds.
V41162	MS8815	2855085-25-3	MS8815 is a selective zeste homolog 2 (EZH2) PROTAC degrader.
V75872	MU1656	2766698-38-6	MU1656 is a potent and specific inhibitor of histone methyltransferase DOT1L with IC50 of 2 nM.
V56083	NSD-IN-2	2351225-46-0	NSD-IN-2 (compound 151) is a potent and irreversible inhibitor of NSD1.
V80020	NSD2-IN-4		NSD2-IN-4 is a potent and specific NSD2-SET inhibitor.
V56088	NSD3-IN-1	347340-51-6	NSD3-IN-1 (compound B1) is an inhibitor (blocker/antagonist) of histone methyltransferase NSD3 with IC50 of 28.58 μM.
V41091	NSD3-IN-2	675190-57-5	NSD3-IN-2 is a potent NSD3 inhibitor (IC50=17.97 μM).
V41089	NSD3-IN-3	445416-12-6	NSD3-IN-3 is a potent NSD3 inhibitor (IC50=1.86 μM).
V2610	OICR-9429	1801787-56-3	OICR-9429 (OICR9429) is a novel, potent and selective antagonist of the interaction between WDR5 and the peptide regions of MLL and Histone 3, disrupting Wdr5-MLL interaction with IC50 of 5 uM.