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CPI-1205 (Lirametostat) is a highly potent (biochemical IC50 = 0.002 μM, cellular EC50 = 0.032 μM) and selective inhibitor of EZH2. CPI-1205 has IC50 values of 2 nM and 52 nM for EZH2 and EZH1, respectively. CPI-1205 selectively inhibits the activity of both wild-type and mutated forms of EZH2, this specifically prevents the methylation of histone H3 on lysine 27 (H3K27). Decrease in histone methylation alters gene expression patterns associated with cancer pathways and results in decreased proliferation of EZH2-expressing cancer cells.
| Molecular Weight | 518.57 |
| Formula | C27H33F3N4O3 |
| CAS Number | 1621862-70-1 |
| 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. |
| 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. |
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Products are for research use only. Not for human use. We do not sell to patients.
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