85-2072-65　eIF2-GTP-tRNAiMet Ternary Complex Inhibitor, BTdCPU (N,N'-diarylurea;translation Initiation Tenrary Complex Inhibitor, 1-(benzo[d][1,2,3]thiadiazol-6-yl)-3-(3,4-dichlorophenyl)urea, BTdCPU, Heme-regulated Inhibitor Kinase Activator, BTdCPU) 10mg　CAS No:1257423-87-2　217337

特徴

• A 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 eIF2a in cells at 10uM 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 175mg/kg, in vivo.
• Synonyms:Heme-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
• Molecular Formula:C₁₃H₈Cl₂N₄OS
• Molecular Weight:339.2
• Appearance:Supplied as a white solid.
• Purity:≥99% (HPLC)
• Solubility:DMSO (25mg/ml, clear, colorless solution)
• Storage and Stability:Lyophilized powder may be stored at -20°C. Stable for 12 months at -20°C. Reconstitute with sterile buffer or dH2O. Aliquot to avoid repeated freezing and thawing. Store at -20°C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.