Catalog No.: PC-24496Not For Human Use, Lab Use Only.
NVP-CGM097 is potent and selective MDM2 inhibitor with Ki of 1.3 nM (human MDM2, HDM2), inhibits p53-MDM2 protein-protein interaction with IC50 of 1.7 nM in TR-FRET assays.
NVP-CGM097 is potent and selective MDM2 inhibitor with Ki of 1.3 nM (human MDM2, HDM2), inhibits p53-MDM2 protein-protein interaction with IC50 of 1.7 nM in TR-FRET assays. NVP-CGM097 is 16-fold more potent on human than dog MDM2 and 51- and 37-fold more potent on human than mouse and rat MDM2, respectively. NVP-CGM097 binds to human MDM2 with an IC50 of 1.7 nM and shows high selectivity over MDM4. NVP-CGM097 is about four times more potent than Nutlin-3a (IC50 = 8.0 nM). NVP-CGM097 significantly redistribute wild-type p53 into the cell nucleus with an IC50 of 0.224 μM. NVP-CGM097 significantly inhibited the proliferation of cells expressing wild-type p53, while sparing the p53 null cells. NVP-CGM097 dose dependently and significantly inhibited SJSA-1 tumor growth in rats.
