Description
A Cdk8 inhibitor (IC50 = 2.6 nM); selective for Cdk8 over a panel of 264 kinases at 1 µM but does inhibit GSK3α (IC50 = 691 nM); inhibits STAT1 phosphorylation in SW620 colorectal cancer cells (IC50 = 8 nM); inhibits Wnt-dependent transcription in LS 174T, COLO 205, and PA-1 cancer cells (IC50s = 32, 9, and 52 nM, respectively, in luciferase reporter assays); reduces tumor growth in a SW620 mouse xenograft model at 50 and 100 mg/kg
Formal name: [(2S)-2-(4-chlorophenyl)-1-pyrrolidinyl](3-methyl-1H-pyrazolo[3,4-b]pyridin-5-yl)-methanone
Synonyms:
Molecular weight: 340.8
CAS: 1883423-59-3
Purity: ≥98%
Formulation: A crystalline solid
