MSC2530818

MSC2530818

CAT N°: 29669
Price:

From 109.00 92.65

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 3? (GSK3?; 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.

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • [(2S)-2-(4-chlorophenyl)-1-pyrrolidinyl](3-methyl-1H-pyrazolo[3,4-b]pyridin-5-yl)-methanone
  • Correlated keywords
    • MSC 2530818 bio available Cdk 8 SW 620 174 T PA1 STAT 1 LS174T COLO205 GSK 3 ?
  • Product Overview:
    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 3? (GSK3?; 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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