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

324892
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Descripción

Replacement Information

Tabla espec. clave

Empirical FormulaCAS #
C₁₃H₈Cl₂N₄OS 1257423-87-2

Products

Número de referenciaEmbalaje Cant./Env.
324892-10MG Frasco de vidrio 10 mg
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
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 Certificados de análisis

CargoNúmero de lote
324892

Referencias bibliográficas

Visión general referencias
Chen, T., et al. 2011. Nat. Chem. Biol. 7, 610.
Ficha técnica

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.