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 CAS No: 1257423-87-2 Molecular Formula: C13H8Cl2N4OS Molecular Weight: 339.2 Purity (NMR): 98% Appearance: White solid 1H-NMR Spectrum: Corresponds to structure Storage and Stability: Store at -20C. Stable for 6 months after receipt.
Molekulargewicht:
339.2
CAS Nummer:
[1257423-87-2]
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