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.
Structure | 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. |