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Beschreibung

A cell-permeable sulfonamidebenzamide derivative that acts as a potent and selective inducer of C/EBP-homologous protein (CHOP, AC50 = 800 nM) without affecting XBP (AC50 >80 &#181,M). Displays a balanced profile in terms of its lipophilic profile (cLogP = 2.7), selectivity, and activation of CHO-CHOP luciferase reporter system. Exhibits high selectivity against a panel of 67 GPCR, nuclear receptors, transporters, and ion channels. Has significantly reduced activity towards dopamine receptor at high concentrations (68% at 10 &#181,M). upregulates the expression of UPR target genes. Displays anti-proliferation properties in wild-type mouse embryonic fibroblasts (EC50 = 4.8 &#181,M), but does not affect CHOP knock out cells even at high concentrations (EC50 >20 &#181,M). Inhibits the proliferation of several cancer cell lines at low micromolar levels. Exhibits favorable pharmacokinetic profile (Cmax = 140 nM, Tmax = 0.17 h at 30 mg/kg, i.p. single dose).