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218719 Casein Kinase I Inhibitor III, PF-4800567 - CAS 1188296-52-7 - Calbiochem

Overview

Key Spec Table

CAS #Empirical Formula
1188296-52-7C₁₇H₁₈ClN₅O₂

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218719-5MG
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      Description
      OverviewA cell-permeable pyrazolopyrimidinylamino compound that acts as a potent, ATP-competitive and reversible inhibitor of CKIε with ~22-fold greater potency over CKIδ (IC50 = 32 and 711 nM, respectively) and displays excellent selectivity among 50-kinases, with the only exception of EGFR (69% inhibition at 1 µM). Shown to preferentially block PER3 (PERIOD3) nuclear translocation in COS7-GFP-PER3-CKIε cells over CKIδ-transfected cells (IC50 = 0.13 and 2.65 µM, respectively), and PER2 degradation in COS7-GFP-PER2-CKIε cells. Unlike Casein Kinase I Inhibitor II, PF-670462 (Cat. No. 218716), PF-4800567 exerts only marginal effect on circadian clock under similar conditions.
      Catalogue Number218719
      Brand Family Calbiochem®
      Synonyms3-(3-Chlorophenoxymethyl)-1-(tetrahydropyran-4-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-ylamine, HCl, CKI Inhibitor III, PF-4800567
      References
      ReferencesMeng, Q.J., et al. 2010. Proc. Natl. Acad. Sci. USA 24, 15240.
      Etchegaray, J.P., et al. 2010. PLoS One 5, e10303.
      Walton, K.M., et al. 2009. J. Pharmacol. Exp. Ther. 330, 430.
      Badura, L., et al. 2007. J. Pharmacol. Exp. Ther. 322, 730.
      Product Information
      CAS number1188296-52-7
      FormBeige solid
      Hill FormulaC₁₇H₁₈ClN₅O₂
      Chemical formulaC₁₇H₁₈ClN₅O₂
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Biological Information
      Purity≥99% by HPLC
      Storage and Shipping Information
      Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
      Toxicity Standard Handling
      Storage +2°C to +8°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 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Global Trade Item Number
      Catalogue Number GTIN
      218719-5MG 04055977218947