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EZH2 EZH2

Inhibitors

Cat.No.  Name Information
M2677 Tazemetostat (EPZ-6438) Tazemetostat (EPZ-6438) is a potent, and selective EZH2 inhibitor with Ki and IC50 of 2.5 nM and 11 nM, exhibiting a 35-fold selectivity versus EZH1 and >4,500-fold selectivity relative to 14 other HMTs.
M13421 PF-06821497 PF-06821497 is a selective and orally active Zeste Homolog 2 (EZH2) inhibitor enhancer with powerful tumor growth inhibition.
M9936 CPI-1205 CPI-1205 is a highly potent (biochemical IC50 = 0.002 μM, cellular EC50 = 0.032 μM) and selective inhibitor of EZH2.
M9914 Valemetostat Valemetostat (DS-3201) is a first-in-class EZH1/2 dual inhibitor, used in the research of relapsed/refractory peripheral T-cell lymphoma.
M9901 MS1943 MS1943 is a pioneering oral bioactive selective EZH2 inhibitor with an IC50 of 120 nM. MS1943 significantly reduced EZH2 protein levels in many triple negative breast and other cancers and non-cancer lines. MS1943 effectively blocked the proliferation of multiple triple negative breast cancers and other cancer lines.
M5027 CPI-169 racemate CPI-169 racemate is the racemate form of CPI-169, which is a novel and potent EZH2 inhibitor with IC50 <1 nM(inhibition of the catalytic activity of PRC2); decreases cellular levels of H3K27me3 with an EC50 of 70 nM, and triggers cell cycle arrest and apoptosis in a variety of cell lines.
M3107 UNC1999 UNC1999 is a potent, orally bioavailable and selective inhibitor of EZH2 and EZH1 with IC50 of 2 nM and 45 nM, respectively, showing >1000-fold selectivity over a broad range of epigenetic and non-epigenetic targets.
M2736 GSK343 GSK343 is a potent and selective EZH2 inhibitor with IC50 of 4 nM, showing 60 fold selectivity against EZH1, and >1000 fold selectivity against other histone methyltransferases.
M2677 Tazemetostat (EPZ-6438) Tazemetostat (EPZ-6438) is a potent, and selective EZH2 inhibitor with Ki and IC50 of 2.5 nM and 11 nM, exhibiting a 35-fold selectivity versus EZH1 and >4,500-fold selectivity relative to 14 other HMTs.
M2676 EPZ005687 EPZ005687 is a potent, selective EZH2 inhibitor,Ki The value is 24 nM, which is 50 times more selective than EZH1 and 500 times more selective than 15 other methyltransferases.
M2114 GSK126 GSK126 is a potent, highly selective, S-adenosyl-methionine-competitive, small-molecule inhibitor of EZH2 methyltransferase activity.



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