SEL120-34A monohydrochloride 是一种ATP-竞争性和选择性的CDK8抑制剂，抑制 CDK8/CycC 和 CDK19/CycC 复合物的活性，IC50值分别为 4.4 nM 和 10.4 nM，对 CDK8 的Kd值为 3 nM。SEL120-34A monohydrochloride 对 CDK9 的作用很弱，计算的IC50值为 1070 nM，而对 CDK1、2、4、6、5、7 等无作用。SEL120-34A monohydrochloride 能够抑制 STAT1 S727 和 STAT5 S726 的磷酸化，具有抗癌活性。

SEL120-34A monohydrochloride is an ATP-competitive and selective CDK8 inhibitor, inhibits kinase activities of CDK8/CycC and CDK19/CycC complexes with IC 50 s of 4.4 nM and 10.4 nM, respectively, with a K d of 3 nM for CDK8. SEL120-34A monohydrochloride weakly inhibits CDK9 (calculated IC 50 =1070 nM) without obvious activity against CDK1, 2, 4, 6, 5, 7. SEL120-34A monohydrochloride inhibits phosphorylation of STAT1 S727 and STAT5 S726 in cancer cells in vitro [1].

SEL120-34A monohydrochloride is an ATP-competitive and selective CDK8 inhibitor, inhibits kinase activities of CDK8/CycC and CDK19/CycC complexes with IC 50 s of 4.4 nM and 10.4 nM, respectively, with a K d of 3 nM for CDK8. SEL120-34A monohydrochloride weakly inhibits CDK9 (calculated IC 50 =1070 nM) without obvious activity against CDK1, 2, 4, 6, 5, 7 [1]. SEL120-34A (1.6 nM-5 μM) inhibits the growth of STAT5 S726 positive KG-1 AML cells while is not cytotoxic to S726 negative MOLM13 AML cells [1]. SEL120-34A monohydrochloride inhibits phosphorylation of STAT1 S727 and STAT5 S726, decreases IRF9 and STAT1 mRNA expression and mitogen-induced IER expression [1].

SEL120-34A monohydrochloride (30, 60 mg/kg, p.o. once every day) inhibits AML tumor growth in SCID mice in a dose-dependent manner after treatment for 17 days [1].

T10744L2

C15H19Br2ClN4

450.6

SEL120-34A monohydrochloride (1609522-33-9 free base)

DMSO:13 mg/mL (28.85 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years