EPZ-719 | SETD2 inhibitor | Probechem Biochemicals

Chemical Structure : EPZ-719

CAS No.: 2697176-16-0

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EPZ-719 (EPZ719)

货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	450.573
分子式	C22H31FN4O3S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	4-Fluoro-7-methyl-N-((1R,3S)-3-((S)-3-(N-methylmethylsulfonamido)pyrrolidin-1-yl)cyclohexyl)-1H-indole-2-carboxamide

参考文献

1. John W Lampe, et al. ACS Med Chem Lett. 2021 Aug 24;12(10):1539-1545.

EPZ-719 (EPZ719)

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物理化学性质&存储条件

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EPZ-719 (EPZ719)

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