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420148 JAK3/GSK-3β/PKCα Inhibitor - CAS 1260181-14-3 - Calbiochem

Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
1260181-14-3C₂₇H₂₅F₃N₄O₄

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420148-5MG
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      Glass bottle 5 mg
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      Description
      OverviewA cell-permeable phenyl-indolyl maleimide compound that acts as a potent, ATP-binding site targeting and reversible inhibitor of GSK-3β, JAK3, PKCα and PKCθ (IC50 = 3, 8, 13 and 68 nM, respectively) with excellent selectivity over 40-kinases, including JAK1, JAK2 and Tyk2 (IC50 = 1.017, 2.55 and 8.055 µM, respectively). Shown to efficiently block interleukin stimulated STAT5 phosphorylation and T cell costimulation (IC50 = 0.525, 1.294 and 0.689 µM in IL15-MO7, IL2-CTLL and TCR/CD28-Jurkat cells, respectively).
      Catalogue Number420148
      Brand Family Calbiochem®
      Synonyms3-(5-(4-(2-Hydroxy-2-methyl-propionyl)-piperazin-1-yl)-2-trifluoromethyl-phenyl)-4-(1H-indol-3-yl)-pyrrole-2,5-dione, NIBR3049, JAK3 Inhibitor XII
      References
      ReferencesHaan, C., et al. 2011. Chem. Biol. 18, 314.
      Thoma, G., et al. 2011. J. Med. Chem. 54, 284.
      Product Information
      CAS number1260181-14-3
      FormYellow solid
      Hill FormulaC₂₇H₂₅F₃N₄O₄
      Chemical formulaC₂₇H₂₅F₃N₄O₄
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Purity≥95% 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 Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
      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 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Catalogue Number GTIN
      420148-5MG 04055977210699

      Documentation

      JAK3/GSK-3β/PKCα Inhibitor - CAS 1260181-14-3 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      JAK3/GSK-3β/PKCα Inhibitor - CAS 1260181-14-3 - Calbiochem Certificates of Analysis

      TitleLot Number
      420148

      References

      Reference overview
      Haan, C., et al. 2011. Chem. Biol. 18, 314.
      Thoma, G., et al. 2011. J. Med. Chem. 54, 284.
      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.

      Revision13-July-2012 JSW
      Synonyms3-(5-(4-(2-Hydroxy-2-methyl-propionyl)-piperazin-1-yl)-2-trifluoromethyl-phenyl)-4-(1H-indol-3-yl)-pyrrole-2,5-dione, NIBR3049, JAK3 Inhibitor XII
      DescriptionA cell-permeable phenyl-indolyl maleimide compound that acts as a potent, ATP-binding site targeting and reversible inhibitor of GSK-3β, JAK3, PKCα and PKCθ (IC50 = 3, 8, 13 and 68 nM, respectively) with excellent selectivity over 40-kinases, including JAK1, JAK2 and Tyk2 (IC50 = 1.017, 2.55 and 8.055 µM, respectively). Shown to efficiently block interleukin stimulated STAT5 phosphorylation and T cell costimulation (IC50 = 0.525, 1.294 and 0.689 µM in IL15-MO7, IL2-CTLL and TCR/CD28-Jurkat cells, respectively).
      FormYellow solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number1260181-14-3
      Chemical formulaC₂₇H₂₅F₃N₄O₄
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO
      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 3 months at -20°C.
      Toxicity Standard Handling
      ReferencesHaan, C., et al. 2011. Chem. Biol. 18, 314.
      Thoma, G., et al. 2011. J. Med. Chem. 54, 284.