420144 JNK Inhibitor XIII - CAS 40045-50-9 - Calbiochem

420144
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₅H₃N₅O₂S₃ 40045-50-9

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      420144-10MG
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          10 mg
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          Description
          OverviewA cell-permeable non-peptidyl thiazolyl-thiadiazole alternative to pepJIP1 (TI-JIP1153-163) and TAT-pepJIP1 (Cat. Nos. 420133 & 420134, respectively) as a JIP-docking site-targeting (IC50 = 239 nM against pepJIP1 binding to JNK1) and substrate-competitive JNK inhibitor (IC50 = 700 nM against ATF2 phosphorylation by JNK1), while exhibiting little activity (IC50 >50 µM) toward p38α, Akt, furin, or lethal factor. Shown to inhibit the phosphorylation of overexpressed GFP-c-Jun in HeLa cultures upon TNF-α stimulation (IC50 = 6.23 µM) in vitro and restore insulin sensitivity in a murine of type-2 diabetes model (25 mg/kg, i.p.) in vivo. Biostability analysis with rat liver microsome preparations results in a compound half-life of 27 min at 37.5°C.
          Catalogue Number420144
          Brand Family Calbiochem®
          Synonyms5-(5-Nitrothiazol-2-ylthio)-1,3,4-thiadiazol-2-amine
          References
          ReferencesDe, S.K., et al. 2009. J. Med. Chem. 52, 1943.
          Product Information
          CAS number40045-50-9
          FormPale yellow solid
          Hill FormulaC₅H₃N₅O₂S₃
          Chemical formulaC₅H₃N₅O₂S₃
          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 with Blue Ice or with Dry Ice
          Toxicity Standard Handling
          Storage -20°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
          420144

          References

          Reference overview
          De, S.K., et al. 2009. J. Med. Chem. 52, 1943.
          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-April-2011 RFH
          Synonyms5-(5-Nitrothiazol-2-ylthio)-1,3,4-thiadiazol-2-amine
          DescriptionA cell-permeable non-peptidyl thiazolyl-thiadiazole alternative to pepJIP1 (TI-JIP1153-163) and TAT-pepJIP1 (Cat. Nos. 420133 & 420134, respectively) as a JIP-docking site-targeting (IC50 = 239 nM against pepJIP1 binding to JNK1) and substrate-competitive JNK inhibitor (IC50 = 700 nM against ATF2 phosphorylation by JNK1), while exhibiting little activity (IC50 >50 µM) toward p38α, Akt, furin, or lethal factor. Shown to inhibit the phosphorylation of overexpressed GFP-c-Jun in HeLa cultures upon TNF-α stimulation (IC50 = 6.23 µM) in vitro and restore insulin sensitivity in a murine of type-2 diabetes model (25 mg/kg, i.p.) in vivo. Biostability analysis with rat liver microsome preparations results in a compound half-life of 27 min at 37.5°C.
          FormPale yellow solid
          Intert gas (Yes/No) Packaged under inert gas
          CAS number40045-50-9
          Chemical formulaC₅H₃N₅O₂S₃
          Structure formulaStructure formula
          Purity≥95% by HPLC
          SolubilityDMSO (50 mg/ml) or Ethanol (4 mg/ml)
          Storage -20°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
          ReferencesDe, S.K., et al. 2009. J. Med. Chem. 52, 1943.