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

MSC2530818 – 5 mg

Brand:
Cayman
CAS:
1883423-59-3
Storage:
-20
UN-No:
Non-Hazardous - /

MSC2530818 is an orally bioavailable cyclin-dependent kinase 8 (Cdk8) inhibitor (IC50 = 2.6 nM).{54067} It is selective for Cdk8 over a panel of 264 kinases at 1 µM but does inhibit glycogen synthase kinase 3α (GSK3α; IC50 = 691 nM). MSC2530818 inhibits STAT1 phosphorylation in SW620 colorectal cancer cells with an IC50 value of 8 nM. It also 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). MSC2530818 (50 and 100 mg/kg) reduces tumor growth in a SW620 mouse xenograft model.  

 

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SKU: 29669 - 5 mg Category:

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

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