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Histone Methyltransferase Histone methyltransferase


Cat.No.  Name Information
M11474 EZM0414 EZM0414 is a potent, selective, oral bioavailable SETD2 inhibitor (IN SETD2 biochemical analysis, IC50=18 nM; In cell analysis, IC50=34 nM). EZM0414 can be used to study relapsed or refractory multiple myeloma and diffuse large B-cell lymphoma.
M11278 GNA002 GNA002 is a potent, selective, covalent EZH2 inhibitor with an IC50 of 1.1 μM against EZH2. GNA002 can specifically and covalently bind Cys668 in the EZH2-SET domain to induce EZH2 degradation through COOH terminal of ubiquitination mediated by Hsp70 interacting protein (CHIP). GNA002 effectively reduced EZH2-mediated H3K27 trimethylation and reactivated tumor suppressor genes silenced by Polycomb repressor complex 2 (PRC2).
M11245 PF-06726304 Pf-06726304 is an effective selective EZH2 inhibitor. Pf-06726304 inhibited wild type and Y641N mutant EZH2 with Ki of 0.7 and 3.0 nM, respectively. Pf-06726304 has strong anti-tumor growth activity.
M11243 CPI-169 Cpi-169 (CPI 169 R-Enantiomer) is a novel and effective EZH2 inhibitor, capable of inhibiting the activity of EZH2 WT, EZH2 Y641N and EZH1 with IC50 value of 0.24 nM, respectively. 0.51 nM and 6.1 nM.
M11242 EI1 EI1 (KB-145943) is a novel and effective EZH2 inhibitor, capable of acting on EZH2 (WT) and EZH2 (Y641F) with IC50 values of 15 nM and 13 nM, respectively.
M11241 Gambogenic acid Gambogenic acid is the active ingredient in Huangteng and has anti-cancer activity. Gambogenic acid is an effective EZH2 inhibitor, which specifically covalently binds to Cys668 in the EZH2-SET domain to induce EZH2 ubiquitination.
M11169 DM-01 DM-01 is a potent and selective EZH2 inhibitor that can be used to study diffuse large B-cell lymphoma (DLBCL), follicular lymphoma (FL), and SNF5/INI-1/SMARCB1 gene-related solid tumors.
M11161 EBI-2511 EBI-2511 is an orally active, potent inhibitor of EZH2 in Pfeffiera cells IC50 The value is 6 nM.
M11055 TP-064 TP-064 is a potent and selective PRMT4 small molecule inhibitor with ic50 < 10 nM, which is more than 100 times more selective for PRMT4 than other PRMT.
M11033 EPZ020411 hydrochloride EPZ020411 hydrochloride is a potent and selective PRMT6 inhibitor, IC50 10 nM, which is more than 10 times more selective than acting on PRMT1 and PRMT8.
M11019 UNC6934 UNC6934 is a chemical probe that targets the PWWP domain of NSD2 and locates kernels.
M10954 MRTX9768 hydrochloride MRTX9768 hydrochloride is a potent, selective, orally active, first-of-its-kind PRMT5-MTA complex inhibitor.
M10953 MRTX-1719 MRTX-1719 is a potent, first-of-its-kind, selective PRMT5/MTA complex inhibitor against PRMT5/MTA MTAPDEL SDMA CELL LINES IC50 The value is <10 nM.
M10952 BRD0639 BRD0639 is a class of inhibitors that inhibit PRMT5-substrate adaptor interaction. BRD0639 is a PRMT5-binding motif (PBM) competitor that supports the study of PBM-dependent PRMT5 activity.
M10951 CMP-5 CMP-5 is a potent and selective PRMT5 inhibitor that is inactive against PRMT1, PRMT4, and PRMT7 enzymes. CMP-5 selectively blocks S2Me-H4R3 by inhibiting PRMT5 methyltransferase activity during histone preparation. CMP-5 blocks EBV-driven B lymphocyte transformation but has no effect on normal B cells.
M10860 MRK-740 MRK-740 is a potent, selective, substrate-competitive PRDM9 histone methyltransferase inhibitor,IC50 80 nM. MRK-740 is more selective to PRDM9 than other histone methyltransferases and other non-epigenetic targets. MRK-740 Reduces PRDM9-Dependent H3K4 Trimethylation (IC50 0.8 μM).
M10532 Tazemetostat hydrobromide Tazemetostat (EPZ-6438) hydrobromide is a potent, selective and orally available EZH2 inhibitor.
M9449 PFI-2 hydrochloride PFI-2 hydrochloride is a potent, highly selective and cell-active inhibitor of the methyltransferase activity of SETD7, with IC50 of 2 nM.
M9442 CM-272 CM-272 is a first-in-class reversible dual small molecule inhibitor against G9a and DNMTs in hematological malignancies.
M9151 MI-503 MI-503 is a potent and selective Menin-MLL inhibitor with IC50 of 14.7 nM.

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