529582 PP1 Analog III, 3-MB-PP1 - CAS 956025-83-5 - Calbiochem

529582
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₁₇H₂₁N₅ 956025-83-5

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      529582-5MG
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          5 mg
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          Description
          OverviewA cell-permeable C3-enlarged PP1 (Cat. No. 567809) analog that is shown to act as a potent, ATP-competitive, and highly ASKA- (analog-sensitive kinase alleles) selective inhibitor against polo-like kinase 1C67V L130G (75% and 94% inhibition in cell-free kinase assays at 0.1 and 1 µM, respectively), ZAP-70C405V M414A/ZAP-70M414A (complete prevention and elimination, respectively, of αTCR-stimulated [Ca2+] elevation in ASKA transfectants when applied before or after αTCR stimulation at 6 µM), and SykM442A S505A (56% inhibition of phagocytosis of Ab-opsonized SRBC by ASKA macrophages at 6 µM), while exhibiting little or no activity toward the wild-type or other off-target cellular enzymes. Functional analog-sensitive allele mutants are valuable tools in pharmacological validation of drug development and in elucidating enzyme signalings and functions both in cultures in vitro and in animals in vivo when specific inhibitors against naturally occurring target enzymes are unavailable and/or generations of knockout animals/cells lacking the target enzymes appear to be difficult, infeasible, or simply impossible.
          Catalogue Number529582
          Brand Family Calbiochem®
          SynonymsSyk ASKA Inhibitor, ZAP-70 ASKA Inhibitor, 1-(tert-Butyl)-3-(3-methylbenzyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine, Plk1 ASKA Inhibitor
          References
          ReferencesMiller, A.L., et al. 2009. J. Immunol. 182, 988.
          Levin, S.E., et al. 2008. J. Biol. Chem. 283, 15419.
          Burkard, M.E., et al. 2007. Proc. Natl. Acad. Sci. USA 104, 4383.
          Bishop, A.C., et al. 1999. J. Am. Chem. Soc. 121, 627.
          Product Information
          CAS number956025-83-5
          FormWhite solid
          Hill FormulaC₁₇H₂₁N₅
          Chemical formulaC₁₇H₂₁N₅
          Structure formula ImageStructure formula Image
          Applications
          ApplicationPP1 Analog III, 3-MB-PP1, CAS 956025-83-5, is a cell-permeable, potent, ATP-competitive, and highly selective inhibitor of polo-like kinase 1C67V L130G and ZAP-70C405V M414A/ZAP-70M414A.
          Biological Information
          Purity≥97% by HPLC
          Physicochemical Information
          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 III, 3-MB-PP1 - CAS 956025-83-5 - Calbiochem SDS

          Title

          Safety Data Sheet (SDS) 

          PP1 Analog III, 3-MB-PP1 - CAS 956025-83-5 - Calbiochem Certificates of Analysis

          TitleLot Number
          529582

          References

          Reference overview
          Miller, A.L., et al. 2009. J. Immunol. 182, 988.
          Levin, S.E., et al. 2008. J. Biol. Chem. 283, 15419.
          Burkard, M.E., et al. 2007. Proc. Natl. Acad. Sci. USA 104, 4383.
          Bishop, A.C., et al. 1999. J. Am. Chem. Soc. 121, 627.
          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.

          Revision23-February-2011 RFH
          SynonymsSyk ASKA Inhibitor, ZAP-70 ASKA Inhibitor, 1-(tert-Butyl)-3-(3-methylbenzyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine, Plk1 ASKA Inhibitor
          DescriptionA cell-permeable C3-enlarged PP1 (Cat. No. 567809) analog that is shown to act as a potent, ATP-competitive, and highly ASKA- (analog-sensitive kinase alleles) selective inhibitor against polo-like kinase 1C67V L130G (75% and 94% inhibition in cell-free kinase assays at 0.1 and 1 µM, respectively), ZAP-70C405V M414A/ZAP-70M414A (complete prevention and elimination, respectively, of αTCR-stimulated [Ca2+] elevation in ASKA transfectants when applied before or after αTCR stimulation at 6 µM), and SykM442A S505A (56% inhibition of phagocytosis of Ab-opsonized SRBC by ASKA macrophages at 6 µM), while exhibiting little or no activity toward the wild-type or other off-target cellular enzymes. Functional analog-sensitive allele mutants are valuable tools in pharmacological validation of drug development and in elucidating enzyme signalings and functions both in cultures in vitro and in animals in vivo when specific inhibitors against naturally occurring target enzymes are unavailable and/or generations of knockout animals/cells lacking the target enzymes appear to be difficult, infeasible, or simply impossible.
          FormWhite solid
          Intert gas (Yes/No) Packaged under inert gas
          CAS number956025-83-5
          Chemical formulaC₁₇H₂₁N₅
          Structure formulaStructure formula
          Purity≥97% by HPLC
          SolubilityDMSO (50 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
          ReferencesMiller, A.L., et al. 2009. J. Immunol. 182, 988.
          Levin, S.E., et al. 2008. J. Biol. Chem. 283, 15419.
          Burkard, M.E., et al. 2007. Proc. Natl. Acad. Sci. USA 104, 4383.
          Bishop, A.C., et al. 1999. J. Am. Chem. Soc. 121, 627.