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

Overview

Replacement Information

Key Specifications Table

Empirical FormulaCAS #
C₅H₃N₅O₂S₃ 40045-50-9

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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
      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 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

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

      Title

      Safety Data Sheet (SDS) 

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