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

420148
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₇H₂₅F₃N₄O₄ 1260181-14-3

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      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
          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

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          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 +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 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.