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

324892
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₁₃H₈Cl₂N₄OS 1257423-87-2

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      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      324892-10MG
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          Glass bottle 10 mg
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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®
          Synonyms1-(benzo[d][1,2,3]thiadiazol-6-yl)-3-(3,4-dichlorophenyl)urea, N,N'-diarylurea;translation initiation tenrary complex inhibitor, heme-regulated inhibitor kinase activator, BTdCPU, BTdCPU
          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
          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

          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
          Synonyms1-(benzo[d][1,2,3]thiadiazol-6-yl)-3-(3,4-dichlorophenyl)urea, N,N'-diarylurea;translation initiation tenrary complex inhibitor, heme-regulated inhibitor kinase activator, BTdCPU, BTdCPU
          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.