[CAS NO. 1346527-98-7]  ML240

ML240 is a potent p97 inhibitor, with an IC ₅₀ of 100 nM. ML240 is active in the UbG76V-GFP stabilization assay (IC ₅₀ , 0.9 μM). ML240 inhibits p97 competitively with respect to ATP with a K _i values of 0.22 μM. ML240 also inhibits labeling of only three protein kinase domains by >50% when tested at 20 μM: PIP5 K3 (belongs to phosphoinositide-3 kinase family), JAK1 JH2 (N-terminal pseudokinase domain of JAK1), and DNAPK (DNA-dependent protein kinase). ML240 (1.1, 3.3, 10, or 20 μM) induces executioner caspases 3 and 7 and triggers cell death independently of apical caspases 8 and 9 ^[1] . ML240 is cytotoxic to HCT15 and SW403 cells, with GI ₅₀ s of 0.76 and 0.5 μM after treatment for 24 h, and 0.54 and 0.5 μM after treatment for 72 h, respectively ^[2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.