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Medchemexpress LLC Romaciclib monohydrochloride | 2443816-41-7 | 99.3% | 450.60 | 25 MG
Supplier: Medchemexpress LLC 25MGHY111388A
Romaciclib monohydrochloride is an ATP-competitive and selective CDK8 inhibitor. It inhibits kinase activities of CDK8/CycC and CDK19/CycC complexes with IC50s of 4.4 nM and 10.4 nM, respectively, and has a Kd of 3 nM for CDK8. It weakly inhibits CDK9 but shows no significant activity against CDK1, 2, 4, 6, 5, or 7. This compound inhibits phosphorylation of STAT1 S727 and STAT5 S726, demonstrating anti-tumor activity.
- ATP-competitive and selective CDK8 inhibitor.
- Inhibits kinase activities of CDK8/CycC and CDK19/CycC complexes.
- Weakly inhibits CDK9 and shows no obvious activity against several other CDKs (CDK1, 2, 4, 6, 5, 7).
- Inhibits phosphorylation of STAT1 S727 and STAT5 S726.
- Possesses anti-tumor activity.
- Decreases IRF9 and STAT1 mRNA expression and mitogen-induced IER expression.
- Inhibits growth of AML tumors in a dose-dependent manner in SCID mice.
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