ML241
p97 AAA ATPase inhibitor / Potent and selective p97 AAA ATPase inhibitor, IC50=100 nM. Inhibits degradation of a p97-dependent but not p97-independent proteasome substrate in a dual-reporter cell line1. It impairs the endoplasmic reticulum-associated degradation (ERAD) pathway.1 ML241 and related inhibitors (DBeQ for example) have differential responses to p97 mutants as well as the presence of cofactors suggesting the possibility of context-dependent p97 inhibitors.2,3
Biochemicals & reagents
1346528-06-0
CID49830260
1) Chou et al. (2013), Structure-activity relationship study reveals ML240 and ML241 as potent and selective inhibitors of p97 ATPase; Chem. Med. Chem., 8 297 2) Chou et al. (2014) Specific inhibition of p97/VCP ATPase amd kinetic analysis demonstrate interaction between D1 and D2 ATPase domains; J. Mol. Biol. 426 2886 3) Fang et al. (2015) Evaluating p97 inhibitor analogues for their domain selectivity and potency against the p97-p47 complex; Chem. Med. Chem. 10 52
-20°C
TARGET: ATPase; ER/Golgi; UPR (Unfolded protein response) -- PATHWAY: Degradation -- RESEARCH AREA: Ubiquitin/Proteasome -- DISEASE AREA: Cancer