ML-291

ML-291 is a novel activator of the apoptotic arm of the unfolded protein response (UPR), but not the adaptive arm.¹ Specifically, it activates signaling through PERK/eIF2α/CHOP (EC₅₀ = 762 nM) but not through IRE1/XBP1 (IC₅₀ > 80 µM).¹ ML-291 induces apoptosis in mouse embryonic fibroblasts overexpressing CHOP (EC₅₀ ~4.8 µM), but not in wild-type or CHOP knockout cells.¹ 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.¹

WARNING This product is not for human or veterinary use.