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Chemical Structure : Pinometostat
CAS No.: 1380288-87-8
Catalog No.: PC-21618Not For Human Use, Lab Use Only.
Pinometostat (EPZ-5676) is a potent and selective inhibitor of DOT1L histone methyltransferase activity with Ki of 0.08 nM, 37000-fold selectivity over other methyltransferases.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg | $158 | In stock | |
| 25 mg | $268 | In stock | |
| 50 mg | $428 | In stock | |
| 100 mg | Get quote |
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Pinometostat (EPZ-5676) is a potent and selective inhibitor of DOT1L histone methyltransferase activity with Ki of 0.08 nM, 37000-fold selectivity over other methyltransferases.
EPZ-5676 occupies the S-adenosyl methionine (SAM) binding pocket and induces conformational changes in DOT1L.
Pinometostat (EPZ-5676) potently inhibits cellular H3K79 methylation with IC50 of 3 nM and 5 nM in MV4-11 and HL60 (non–MLL-rearranged) cells, respectively, inhibits MLL-fusion target gene expression.
Pinometostat (EPZ-5676) selectively inhibits proliferation of MLL-rearranged leukemia cells with IC50 of 3.5 nM (MV4-11 proliferation), demonstrates nanomolar antiproliferative activity against most of the MLL-rearranged cell lines, but not non-MLL-rearranged cell lines.
EPZ-5676 (70 mg/kg) causes complete and sustained regression in rodent subcutaneous (SC) MV4-11 xenograft models.
| M.Wt | 562.72 | |
| Formula | C30H42N8O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
(2R,3R,4S,5R)-2-(6-Amino-9H-purin-9-yl)-5-(((cis-3-(2-(5-(tert-butyl)-1H-benzo[d]imidazol-2-yl)ethyl)cyclobutyl)(isopropyl)amino)methyl)tetrahydrofuran-3,4-diol |
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1. Daigle SR, et al. Blood. 2013 Aug 8;122(6):1017-25.
2. Klaus CR, et al. J Pharmacol Exp Ther. 2014 Sep;350(3):646-56.
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