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422000 Kenpaullone - CAS 142273-20-9 - Calbiochem

Overview

Key Spec Table

CAS #Empirical Formula
142273-20-9C₁₆H₁₁BrN₂O

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422000-1MGCN
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      Description
      OverviewA potent, cell-permeable, and reversible inhibitor of glycogen synthase kinase-3β (IC50 = 230 nM), Lck (IC50 = 470 nM), and cyclin-dependent kinases (Cdks). Inhibits Cdk1/cyclin B (IC50 = 400 nM), Cdk2/cyclin A (IC50 = 680 nM), Cdk2/cyclin E (IC50 = 7.5 µM), and Cdk5/p25 (IC50 = 850 nM). Also inhibits other kinases such as c-Src (IC50 = 15 µM), casein kinase II (IC50 = 20 µM), ERK1 (IC50 = 20 µM), and ERK2 (IC50 = 9 µM). Inhibition is competitive with respect to ATP binding.
      Catalogue Number422000
      Brand Family Calbiochem®
      Synonyms9-Bromo-7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one, NSC-664704
      References
      ReferencesBain, J., et al. 2003. Biochem. J. 371, 199.
      Buolamwini, J.K. 2000. Curr. Pharm. Des. 6, 379.
      Schultz, C., et al. 1999. J. Med. Chem. 42, 2909.
      Zaharevitz, D.W., et al. 1999. Cancer Res. 59, 2566.
      Product Information
      CAS number142273-20-9
      ATP CompetitiveY
      FormYellow-brown solid
      Hill FormulaC₁₆H₁₁BrN₂O
      Chemical formulaC₁₆H₁₁BrN₂O
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Biological Information
      Primary TargetGsk-3β
      Primary Target IC<sub>50</sub>230 nM, 470 nM, 400 nM, 680 nM, 7.5 µM, 850 nM, 15 µM, 20 µM, 20 µM, 9 µM against glycogen synthase kinase-3β, Lck IC50, Cdk1/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E, and Cdk5/p25, c-Src, casein kinase II, ERK1, and ERK2
      Purity≥95% by HPLC
      Physicochemical Information
      Cell permeableY
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage -20°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Global Trade Item Number
      Catalogue Number GTIN
      422000-1MGCN 04055977187137