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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
MM-102 V0400 MM-102 1417329-24-8 MM-102 (also known as HMTase Inhibitor IX) is a novel and potent peptidomimetic inhibitor of MLL1 (Mixed lineage leukemia 1) with anticancer activity.
MM-102 TFA V32086 MM-102 TFA 1883545-52-5 MM-102 TFA (the trifluoroacetic acid salt of MM-102) is a novel, potent,high-affinity peptidomimeticMLL1inhibitor withIC50of 0.4 μM in a cell-free assay.
MM-401 V22884 MM-401 1442106-10-6 MM-401 is a novel, potent and selective inhibitor of histone H3K4 methyltransferase MLL1 activity.
MM-589 TFA V41182 MM-589 TFA 2253167-09-6 MM-589 TFA is a potent inhibitor of WD repeat domain 5 (WDR5) and mixed lineage leukemia (MLL) protein-protein interactions.
MRTX-1719 hydrochloride 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.
MRTX9768 hydrochloride V76744 MRTX9768 hydrochloride MRTX9768 HCl is a potent, selective, orally bioactive, first-in-class inhibitor of the PRMT5-MTA complex.
MS-023 trihydrochloride 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.
MS-33 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.
MS-67 V51748 MS-67 2407452-77-9 MS67 is a potent and specific WD40 repeat domain protein 5 (WDR5) degrader with Kd of 63 nM.
MS023 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.
MS023 二盐酸盐 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.
MS049 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.
MS049 2HCl 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.
MS117 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.
MS152 V101463 MS152 MS152 is an oral, bioactive EHMT2/G9a inhibitor that reactivates the maternally silenced PWS gene in brain and liver tissues in a mouse model of Prader-Willi syndrome (PWS).
MS1943 V40191 MS1943 2225938-17-8 MS1943 (MS-1943) is a novel and potent EZH2 degrader(IC50 = 120 nM) with anticancer activity.
MS8511 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.
MS8511 hydrochloride V103386 MS8511 hydrochloride 3031788-28-7 MS8511 (hydrochloride) is a selective, covalent, irreversible G9a/GLP inhibitor targeting the cysteine residue in the substrate binding site, with IC50 values of 100 nM (G9a) and 140 nM (GLP), and Kd values of 44 nM (G9a) and 46 nM (GLP).
MS8815 V41162 MS8815 2855085-25-3 MS8815 is a selective zeste homolog 2 (EZH2) PROTAC degrader.
MS8847 V83609 MS8847
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