ML-291 is a novel activator of the apoptotic arm of the unfolded protein response (UPR), but not the adaptive arm. Specifically, it activates signaling through PERK/eIF2α/CHOP (EC = 762 nM) but not through IRE1/XBP1 (IC > 80 µM). ML-291 induces apoptosis in mouse embryonic fibroblasts overexpressing CHOP (EC ~4.8 µM), but not in wild-type or CHOP knockout cells. It has minimal activity against a panel of 67 receptors, ion channels, and transporters, with the exception of the dopamine transporter (68% inhibition). ML-291 displays greater than average antitumor cell cytotoxicity against colon, melanoma, and renal cancer cell lines in an NCI-60 panel.
ML291 is a UPR (unfolded protein response)-inducing sulfonamidebenzamide. ML291 overwhelms the adaptive capacity of the UPR and induces apoptosis in a variety of solid cancer models. ML291 can activate the PERK/eIF2a/CHOP (apoptotic) arm of the UPR and reduce leukemic cell burden.
分子式
C16H16ClN3O6S
分子量
413.8
CAS号
1523437-16-2
中文名称
ML291
运输条件
Room temperature in continental US; may vary elsewhere.