SEL120-34A monohydrochloride 是一种选择性的，ATP-竞争性的 CDK8 抑制剂，对 CDK8/CycC 和 CDK19/CycC 复合物的 IC₅₀ 值分别为 4.4 nM 和 10.4 nM，对 CDK8 的 K_d 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。具有抗肿瘤活性。

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), but shows no obvious activity against CDK1, 2, 4, 6, 5, 7. SEL120-34A monohydrochloride inhibits phosphorylation of STAT1 S727 and STAT5 S726. Has anti-tumor activity.

Solid

CDK8/CycC 4.4 nM (IC50) CDK19/CycC 10.4 nM

SEL120-34A monohydrochloride is an ATP-competitive and selective CDK8 inhibitor, inhibits kinase activities of CDK8/CycC and CDK19/CycC complexes with IC50s of 4.4 nM and 10.4 nM, respectively, with a Kd of 3 nM for CDK8. SEL120-34A monohydrochloride weakly inhibits CDK9 (calculated IC50=1070 nM), but shows no obvious activity against CDK1, 2, 4, 6, 5, 7.
SEL120-34A (1.6 nM-5 μM) inhibits the growth of STAT5 S726 positive KG-1 AML cells, but is not cytotoxic to S726 negative MOLM13 AML cells.
SEL120-34A monohydrochloride inhibits phosphorylation of STAT1 S727 and STAT5 S726, decreases IRF9 and STAT1 mRNA expression and mitogen-induced IER expression. has not independently confirmed the accuracy of these methods. They are for reference only.

SEL120-34A monohydrochloride (30, 60 mg/kg, p.o. once every day) inhibits growth of AML tumors in a dose-dependent manner in SCID mice after treatment for 17 days. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

[1]. Rzymski T, et al. SEL120-34A is a novel CDK8 inhibitor active in AML cells with high levels of serine phosphorylation of STAT1 and STAT5 transactivation domains. Oncotarget. 2017 May 16;8(20):33779-33795.

In Vitro: H₂O : 50 mg/mL (110.96 mM; Need ultrasonic)DMSO : 16.67 mg/mL (37.00 mM; ultrasonic and warming and heat to 60°C)配制储备液