ML-240

ML-240 is an ATP-competitive inhibitor of the D2 domain of the ATPase p97 (IC₅₀ = 0.11 µM; K_i = 0.22 µM).^1,2 It disrupts the endoplasmic reticulum-associated degradation (ERAD) and autophagy pathways, preventing the degradation of p97-dependent proteasome substrates (IC₅₀ = 0.9 µM) and causing accumulation of ubiquitin conjugates in nuclear membrane and cytosolic compartments at 5-10 µM.¹ ML-240 has also been shown to block proliferation of HCT15 and SW403 colon cancer cell lines (GI₅₀s = 0.76 and 0.5 µM, respectively) and to rapidly mobilize caspase-3 and -7, inducing apoptosis.¹

WARNING This product is not for human or veterinary use.

1. Chou, T.F., Li, K., Frankowski, K.J., et al. Structure-activity relationship study reveals ML240 and ML241 as potent and selective inhibitors of p97 ATPase. ChemMedChem 8(2), 297-312 (2013).

2. Chou, T.F., Bulfer, S.L., Weihl, C.C., et al. Specific inhibition of p97/VCP ATPase and kinetic analysis demonstrate interaction between D₁ and D₂ ATPase domains. J. Mol. Biol. 426(15), 2886-2899 (2014).