|Description||NMS-859 is very selective (IC50 >10 μM) against all of the AAA ATPases, HSP90 or the 53 kinases tested. NMS-859 was active in a cell proliferation assay, with IC50 values of 3.5 μM and 3.0 μM in HCT116 and HeLa cell lines, respectively. NMS-859 covalently modifies VCP on the active site Cys522 and blocks ATP binding. NMS-859 provided critical validation of VCP as a cancer target, and it raises the possibility that targeting VCP might prevent proteasome inhibitor–resistant tumors from escaping through the aggresome-autophagy pathways and cause them to collapse under the high load of unfolded proteins.|
NMS-859 is very selective (IC50 >10 μM) against all of the AAA ATPases, HSP90 or the 53 kinases tested. NMS-859 was active in a cell proliferation assay, with I...
ML240, a quinazoline derivative, has been found to be a p97 ATPase inhibitor and probably be effective against colon cancer and show antiproliferative activity ...
ML241 is identified as a potent and selective inhibitors of p97 ATPase (IC(50)= 100 nM). ML241 inhibits degradation of a p97-dependent but not a p97-independent...
This active molecular is a selective p97 inhibitor. The IC50 value of it decreased with increasing ATP concentration. IC50 value is 26.0 ± 0.9μM in 5μM ATP, 11....
CB-5083 is a novel first in class, potent orally bio-available p97 inhibitor that disrupts cellular protein homeostasis and demonstrates anti-tumor activity in ...
DBeQ inhibits p97 competitively with respect to ATP, with Ki of 3.2 μM, suggesting that it binds to the active site of the D2 domain.