| 产品描述: | IRE1 抑制剂;IRE1 Inhibitors;;InformationMKC-3946 MKC3946 is a potent and soluble IRE1α endoribonuclease domain inhibitor which triggered modest growth inhibition in multiple myeloma cell lines, without toxicity in normal mononuclear cells.TargetsIRE1α endoribonucleaseIn vitroMKC-3946 triggers modest growth inhibition in MM cell lines, without toxicity in normal mononuclear cells. Importantly, it significantly enhances cytotoxicity induced by bortezomib or 17-AAG, even in the presence of bone marrow stromal cells or exogenous IL-6. Both bortezomib and 17-AAG induce ER stress, evidenced by induction of XBP1s, which is blocked by MKC-3946. Apoptosis induced by these agents is enhanced by MKC-3946, associated with increased CHOP. MKC-3946 treatment does not inhibit IRE1α kinase function or binding of activated IRE1α to TRAF2 and downstream JNK signaling.In vivoMKC-3946 inhibits XBP1 splicing in a model of ER stress associated with significant growth inhibition of MM cells.Cell Research(from reference)Cell lines:RPMI 8226 cells Concentrations:2.5, 5, 10 μM Incubation Time:3 hours |