MKC-3946 (C007B-231338)

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.

Specifications and Purity: 10mM in DMSO

Molecular Formula: C21H20N2O3S

Molecular Weight: 380.46

PubChem CID: 59599728

Isomeric SMILES: CN1CCN(CC1)C(=O)C2=CC=C(S2)C3=CC4=C(C=C3)C(=C(C=C4)O)C=O