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

529581
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Overview

Replacement Information

Key Spec Table

Empirical FormulaCAS #
C₂₀H₂₁N₅221244-14-0

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529581-1MGCN
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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
      Applications
      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
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      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
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      PP1 Analog II, 1NM-PP1 - CAS 221244-14-0 - Calbiochem Certificates of Analysis

      TitleLot Number
      529581

      References

      Reference overview
      Ira, 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.

      Citations

      Title
    • Meenalakshmi M. Mariappan, et al. (2005) Phospholipase Cγ-Erk Axis in Vascular Endothelial Growth Factor-Induced Eukaryotic Initiation Factor 4E Phosphorylation and Protein Synthesis in Renal Epithelial Cells. Journal of Biological Chemistry 280, 28402-28411.
    • Data Sheet

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision10-October-2007 JSW
      SynonymsMutant Kinases Inhibitor II, 4-Amino-1-tert-butyl-3-(1ʹ-naphthylmethyl)pyrazolo[3,4-d]pyrimidine, NM
      DescriptionA cell-permeable and reversible PP1 analog (Cat. No. 529579) that acts as a potent, selective, and ATP-competitive inhibitor of mutant kinases compared to the corresponding wild-type kinase (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.
      FormWhite solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number221244-14-0
      Chemical formulaC₂₀H₂₁N₅
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO (5 mg/ml)
      Storage +2°C to +8°C
      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.
      Toxicity Standard Handling
      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.
      Citation
    • Meenalakshmi M. Mariappan, et al. (2005) Phospholipase Cγ-Erk Axis in Vascular Endothelial Growth Factor-Induced Eukaryotic Initiation Factor 4E Phosphorylation and Protein Synthesis in Renal Epithelial Cells. Journal of Biological Chemistry 280, 28402-28411.