SEL120-34A monohydrochloride |
| Katalog-Nr.GC34355 |
SEL120-34A-Monohydrochlorid ist ein ATP-kompetitiver und selektiver CDK8-Inhibitor, der die KinaseaktivitÄten von CDK8/CycC- und CDK19/CycC-Komplexen mit IC50s von 4,4 nM bzw. 10,4 nM hemmt, mit einem Kd von 3 nM fÜr CDK8. SEL120-34A-Monohydrochlorid hemmt CDK9 schwach (berechneter IC50 = 1070 nM), zeigt aber keine offensichtliche AktivitÄt gegen CDK1, 2, 4, 6, 5, 7. SEL120-34A-Monohydrochlorid hemmt die Phosphorylierung von STAT1 S727 und STAT5 S726. Hat Anti-Tumor-AktivitÄt.
Products are for research use only. Not for human use. We do not sell to patients.
Sample solution is provided at 25 µL, 10mM.
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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 monohydrochloride inhibits phosphorylation of STAT1 S727 and STAT5 S726[1]. Has anti-tumor activity[1].
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[1].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[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 growth of AML tumors in a dose-dependent manner in SCID mice after treatment for 17 days[1].
[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.
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