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Chemical Structure : EPZ-719
CAS No.: 2697176-16-0
Catalog No.: PC-72317Not For Human Use, Lab Use Only.
EPZ-719 (EPZ 719) is a potent, selective SETD2 histone methyltransferase inhibitor with IC50 of 8 nM.
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EPZ-719 (EPZ 719) is a potent, selective SETD2 histone methyltransferase inhibitor with IC50 of 8 nM.
EPZ-719 displayed a >8000-fold selectivity in a panel of 14 other histone methyltransferases, showing a remarkable level of selectivity over these closely related and potentially confounding targets.
EPZ-719 demonstrated the activity in a cellular context using an in-cell Western (ICW) cell biochemical assay in A549 cells by monitoring the H3K36 trimethyl mark with IC50 of 23 nM.
EPZ-719 potent antiproliferative activity against multiple myeloma cell lines, KMS34 and KMS1, with LTP day 14 IC50 of 25 nM and 211 nM.
EPZ-719 is an attractive tool compound for the interrogation of SETD2 biology that enables in vivo target validation studies.
| M.Wt | 450.573 | |
| Formula | C22H31FN4O3S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
4-Fluoro-7-methyl-N-((1R,3S)-3-((S)-3-(N-methylmethylsulfonamido)pyrrolidin-1-yl)cyclohexyl)-1H-indole-2-carboxamide |
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1. John W Lampe, et al. ACS Med Chem Lett. 2021 Aug 24;12(10):1539-1545.
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