ML240

ML240 is a potent p97 inhibitor, inhibiting p97 ATPase with IC₅₀ value of 100 nM. IC50 & Target:IC50: 100 nM (p97)^[1] In Vitro:ML240 is a potent p97 inhibitor, with an IC₅₀ of 100 nM. ML240 is active in the UbG76V-GFP stabilization assay (IC₅₀, 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 GI₅₀s 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].