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

PP1 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.

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Synonyme: 1-(tert-Butyl)-3-(3-methylbenzyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine, Plk1 ASKA Inhibitor, Syk ASKA Inhibitor, ZAP-70 ASKA Inhibitor

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529582
Preis & Verfügbarkeit

Übersicht

Replacement Information

Key Spec Table

CAS #Empirical Formula
956025-83-5C₁₇H₂₁N₅

Preis & Verfügbarkeit

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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®
      Synonyms1-(tert-Butyl)-3-(3-methylbenzyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine, Plk1 ASKA Inhibitor, Syk ASKA Inhibitor, ZAP-70 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
      Quality LevelMQ100
      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
      Global Trade Item Number
      Bestellnummer GTIN
      529582-5MG 04055977269888

      Documentation

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

      Titel

      Sicherheitsdatenblatt (SDB) 

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

      TitelChargennummer
      529582

      Literatur

      Übersicht
      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.
      Datenblatt

      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
      Synonyms1-(tert-Butyl)-3-(3-methylbenzyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine, Plk1 ASKA Inhibitor, Syk ASKA Inhibitor, ZAP-70 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 Protect from light
      +2°C to +8°C
      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.