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

      Pricing & Availability

      Catalogue NumberAvailability Packaging Qty/Pack Price Quantity
      529581-1MG
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          Glass bottle 1 mg
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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
          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

          SDS

          Title

          Safety Data Sheet (SDS) 

          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.