| Cat.No. | Name | Information |
|---|---|---|
| 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. |
| M13421 | PF-06821497 | PF-06821497 is a selective and orally active Zeste Homolog 2 (EZH2) inhibitor 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, DS-3201b) is a first-in-class dual inhibitor targeting EZH1 and EZH2. It can be used in the study of adult T-cell leukemia/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. |
| 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. |
| 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. |
| M50204 | Tulmimetostat | Tulmimetostat is an orally active dual EZH1/EZH2 protein inhibitor with antitumor activity for use in a variety of solid tumor studies. |
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