EPZ031686 产品说明书 Chemicals
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产品编号 DC10887
名称 EPZ031686

化学性质

CAS 1808011-22-4
分子式 C26H34CLF3N4O4S
分子量 591.09
存储条件 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

生物活性

Description
In Vivo
In Vitro

化合物的使用

Kinase Assay
Cell Assay
Animal Administration

参考文献


EPZ031686 is a noncompetitive inhibitor for SMYD3 and MEKK2 with a Ki=1.2 and 1.1 nM respectively. In vitro: EPZ031686 have a cellular potency at a level sufficient to probe the in vitro biology of SMYD3 inhibition. The first SMYD3 inhibitor identify to show double-digit nanomolar cellular activity. EPZ031686 show < 30% inhibition against 16 histone methyltransferase targets at a 10 uM screening concentration. In vivo: EPZ031686 show good bioavailability following oral dosing in mice. The administration for mice is 1 mg/kg by i.v.
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