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529581 PP1 Analog II, 1NM-PP1 - CAS 221244-14-0 - Calbiochem

Overview

Key Spec Table

CAS #Empirical Formula
221244-14-0C₂₀H₂₁N₅

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529581-1MG
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      Description
      OverviewA cell-permeable and reversible PP1 analog (Cat. No. 529579) that acts as a potent and selective ATP-competitive inhibitor of mutant kinases over wild-type (IC50 = 3.2 nM for T339G, c-Fyn-as1 vs. 1.0 µM for c-Fyn; 4.3 nM for I338G, v-src-as1 vs. 28 µM for v-src; 5 nM for F80G, CDK2-as1 vs. 29 µM for CDK2; 8 nM for F89G, CAMK IIα-as1 vs. 24 µM for CAMKII; 120 nM for T315A, c-Abl-as2 vs. 3.4 µM for c-Abl). Shown to activate mutants of Ire1, a transmembrane kinase. Also available as a 10 mM solution in DMSO (Cat. No. 529606).
      Catalogue Number529581
      Brand Family Calbiochem®
      SynonymsMutant Kinases Inhibitor II, 4-Amino-1-tert-butyl-3-(1ʹ-naphthylmethyl)pyrazolo[3,4-d]pyrimidine, NM
      References
      ReferencesIra, G., et al. 2004. Nature 431, 1011.
      Papa, F.R., et al. 2003. Science 302, 1533.
      Bishop, A.C., et al. 2000. Nature 407, 395.
      Weiss, E.L., et al. 2000. Nat. Cell Biol. 2, 677.
      Bishop, A.C., et al. 1999. J. Am. Chem. Soc. 121, 627.
      Product Information
      CAS number221244-14-0
      ATP CompetitiveY
      FormWhite solid
      Hill FormulaC₂₀H₂₁N₅
      Chemical formulaC₂₀H₂₁N₅
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Biological Information
      Primary TargetT339G
      Primary Target IC<sub>50</sub>3.2 nM for T339G, c-Fyn-as1 vs. 1.0 µM for c-Fyn; 4.3 nM for I338G, v-src-as1 vs. 28 µM for v-src; 5 nM for F80G, CDK2-as1 vs. 29 µM for CDK2; 8 nM for F89G, CAMK IIα-as1 vs. 24 µM for CAMKII; 120 nM for T315A, c-Abl-as2 vs.
      Purity≥95% by HPLC
      Physicochemical Information
      Cell permeableY
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      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
      529581-1MG 04055977269871