|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.|
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....
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 ...
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.
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...
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 ...