MKC8866

MKC8866 is an inhibitor of inositol-requiring enzyme 1alpha (IRE1alpha) RNase activity (IC50 = 0.29 µM). It inhibits DTT-induced production of the IRE1alpha target protein and transcription factor X-box binding protein 1 (XBP1) in MM.1S multiple myeloma cells (EC50 = 0.52 µM) and XBP1 production induced by thapsigargin (Cay-10522) in LNCaP cells (IC50 = 0.38 µM). MKC8866 also decreases expression of the XBP1 target genes SREBF1, DGAT2, and LIPE and increases triglyceride levels in MDA-MB-231 cells. In vivo, MKC8866 (300 mg/kg) reduces tumor volume in LNCaP, VCaP, 22Rv1, and C4-2B prostate cancer mouse xenograft models.Formal Name: 7-hydroxy-6-methoxy-4-methyl-3-[2-(4-morpholinyl)-2-oxoethyl]-2-oxo-2H-1-benzopyran-8-carboxaldehyde. CAS Number: 1338934-59-0. Synonyms: IRE1-IN-8866, Inositol-Requiring Enzyme 1alpha Inhibitor 8866. Molecular Formula: C18H19NO7. Formula Weight: 361.4. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 1 mg/ml. lambdamax: 259, 288, 324, 367 nm. SMILES: O=CC1=C(C(OC)=CC2=C1OC(C(CC(N3CCOCC3)=O)=C2C)=O)O. InChi Code: InChI=1S/C18H19NO7/c1-10-11-7-14(24-2)16(22)13(9-20)17(11)26-18(23)12(10)8-15(21)19-3-5-25-6-4-19/h7,9,22H,3-6,8H2,1-2H3. InChi Key: IFDGMRMUJYGWQQ-UHFFFAOYSA-N.