MKC-3946

MKC-3946 is an inhibitor of inositol-requiring enzyme 1alpha (IRE1alpha). It inhibits basal XBP1 splicing, a marker of IRE1alpha activity, in RPMI 8226 multiple myeloma cells in a concentration-dependent manner. MKC-3946 also inhibits XBP1 splicing induced by endoplasmic reticulum (ER) stress and reduces expression of the XBP1 target genes SEC61A1, p58IPK, and ERdj4 in RPMI 8226 cells. In vitro, it is cytotoxic to multiple myeloma cell lines but has no effect on normal mononuclear cells. In vivo, MKC-3946 (100 mg/kg) reduces tumor growth and XBP1 splicing in an RPMI 8226 mouse xenograft model.Formal Name: 2-hydroxy-6-[5-[(4-methyl-1-piperazinyl)carbonyl]-2-thienyl]-1-naphthalenecarboxaldehyde. CAS Number: 1093119-54-0. Molecular Formula: C21H20N2O3S. Formula Weight: 380.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMF:PBS (pH 7.2) (1:6): 0.14 mg/ml, DMSO: 14 mg/ml. lambdamax: 226, 316 nm. SMILES: O=C([H])C1=C2C(C=C(C3=CC=C(C(N4CCN(C)CC4)=O)S3)C=C2)=CC=C1O. InChi Code: InChI=1S/C21H20N2O3S/c1-22-8-10-23(11-9-22)21(26)20-7-6-19(27-20)15-2-4-16-14(12-15)3-5-18(25)17(16)13-24/h2-7,12-13,25H,8-11H2,1H3. InChi Key: IVQVBMWPWPTSNO-UHFFFAOYSA-N.