Formulation: A solid
Formal Name: 7-hydroxy-6-methoxy-4-methyl-3-[2-(4-morpholinyl)-2-oxoethyl]-2-oxo-2H-1-benzopyran-8-carboxaldehyde
Purity: ≥98%
Formula Markup: C18H19NO7
Formula Weight: 361,4
Shelf life (days): 1460
CAS Number: 1338934-59-0
Notes: MKC8866 is an inhibitor of inositol-requiring enzyme 1α (IRE1α) RNase activity (IC50 = 0.29 µM).{67243} It inhibits DTT-induced production of the IRE1α 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 (Item No. 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.{67244} In vivo, MKC8866 (300 mg/kg) reduces tumor volume in LNCaP, VCaP, 22Rv1, and C4-2B prostate cancer mouse xenograft models.{67243}