324892 eIF2-GTP-tRNAiMet ternary complex Inhibitor, BTdCPU - CAS 1257423-87-2 - Calbiochem

324892
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Empirical FormulaCAS #
C₁₃H₈Cl₂N₄OS 1257423-87-2

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324892-10MG
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      Description
      OverviewA cell-permeable N, N'-diarylurea that acts as an inhibitor of the formation of the ternary complex of eukaryotic translation initiation factor 2 (eIF2), GTP and the initiator methionine tRNA (Met-tRNAi), a key regulatory step of translation initiation. It directly activates heme-regulated inhibitor kinase (HRI), which then phosphorylates eIF2α in cells at 10 µM and in cell-free extracts dose-dependently, and thereby prevents respective ternary complex formation without elevating oxidative stress. The sensitivities of various cancer cell lines to the anti-proliferative effects of this compound are shown to correlate with the expression of HRI. Furthermore, this compound displays tumor growth inhibition in a mice xenograft model of MCF-7 human breast cancer cells at 175 mg/kg, in vivo.
      Catalogue Number324892
      Brand Family Calbiochem®
      Synonymsheme-regulated inhibitor kinase activator, BTdCPU, BTdCPU, 1-(benzo[d][1,2,3]thiadiazol-6-yl)-3-(3,4-dichlorophenyl)urea, N,N'-diarylurea;translation initiation tenrary complex inhibitor
      References
      ReferencesChen, T., et al. 2011. Nat. Chem. Biol. 7, 610.
      Product Information
      CAS number1257423-87-2
      FormWhite solid
      Hill FormulaC₁₃H₈Cl₂N₄OS
      Chemical formulaC₁₃H₈Cl₂N₄OS
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Purity≥99% 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 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      eIF2-GTP-tRNAiMet ternary complex Inhibitor, BTdCPU - CAS 1257423-87-2 - Calbiochem Certificates of Analysis

      TitleLot Number
      324892

      References

      Reference overview
      Chen, T., et al. 2011. Nat. Chem. Biol. 7, 610.
      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.

      Revision27-June-2012 JSW
      Synonymsheme-regulated inhibitor kinase activator, BTdCPU, BTdCPU, 1-(benzo[d][1,2,3]thiadiazol-6-yl)-3-(3,4-dichlorophenyl)urea, N,N'-diarylurea;translation initiation tenrary complex inhibitor
      DescriptionA cell-permeable N,N'-diarylurea that acts as an inhibitor of the formation of the ternary complex of eukaryotic translation initiation factor 2 (eIF2), GTP and the initiator methionine tRNA (Met-tRNAi), a key regulatory step of translation initiation. It directly activates heme-regulated inhibitor kinase (HRI), which then phosphorylates eIF2α in cells at 10 µM and in cell-free extracts dose-dependently, and thereby prevents respective ternary complex formation without elevating oxidative stress. The sensitivities of various cancer cell lines to the anti-proliferative effects of this compound are shown to correlate with the expression of HRI. Furthermore, this compound displays tumor growth inhibition in a mice xenograft model of MCF-7 human breast cancer cells at 175 mg/kg, in vivo.
      FormWhite solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number1257423-87-2
      Chemical formulaC₁₃H₈Cl₂N₄OS
      Structure formulaStructure formula
      Purity≥99% by HPLC
      SolubilityDMSO (25 mg/ml; clear, colorless solution)
      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
      ReferencesChen, T., et al. 2011. Nat. Chem. Biol. 7, 610.