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

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1.Flaherty, D.P.,Golden, J.E.,Liu, C., et al. Selective small molecule activator of the apoptotic arm of the UPR. Probe Reports from the NIH Molecular Libraries Program (2012).