|Description||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 solid and hematological models . CB-5083 causes rapid and sustained accumulation of poly-ubiquitin in tumor xenografts after a single administration. CB-5083 showed activity to inhibit tumor growth in multiple rodent models of human cancer. Furthermore, CB-5083 appears to exhibit greater potency over current proteasome inhibitors that further validate targeting p97 and protein homeostasis in the treatment of cancer.|
|Synonyms||CB5083; CB-5083; CB 5083.|
|Quality Standard||Enterprise Standard|
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 ...
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...
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.
ML240, a quinazoline derivative, has been found to be a p97 ATPase inhibitor and probably be effective against colon cancer and show antiproliferative activity ...
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...
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....