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CPI-169, a representative compound from that effort, inhibits the catalytic activity of PRC2 with an IC50 of < 1nM, decreases cellular levels of H3K27me3 with an EC50 of 70 nM, and triggers cell cycle arrest and apoptosis in a variety of cell lines. Importantly, compound treatment triggers a sequence of downstream functional consequences of EZH2 inhibition whereby apoptosis is not induced before ten days of continuous target engagement.
| Molecular Weight | 528.66 |
| Formula | C27H36N4O5S |
| CAS Number | 1450655-76-1 |
| Solubility (25°C) | DMSO > 80 mg/ml |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related EZH2 Products |
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| GSK126
GSK126 is a potent, highly selective, S-adenosyl-methionine-competitive, small-molecule inhibitor of EZH2 methyltransferase activity. |
| 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. |
| 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. |
| 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. |
| 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. |
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