|Description||AMG232 is an extremely potent MDM2 inhibitor with remarkable pharmacokinetic properties and in vivo antitumor activity in the SJSA-1 osteosarcoma xenograft model (ED50 = 9.1 mg/kg). AMG232 is currently under clinical development.|
|Synonyms||AMG-232; AMG 232.|
Nutlin-3 is MDM2 antagonist, inhibits p53-Mdm2 interaction (IC50=0.09 µM).
NVP-CGM097 sulfate, a dihydroisoquinolinone derivative, is a potent and selective MDM2 inhibitor (IC50= 1.7±0.1 nM for hMDM2) in the treatment of p53wt tumors.
Nutlin-3a is an inhibitor of MDM2 (human homolog of murine double minute 2), which disrupts its interaction with p53, leading to the stabilization and activatio...
Idasanutlin; also known as RG7388 and RO5503781, is a highly potent and selective MDM2 antagonist with potential anticancer activity. RG7388 binds to MDM2 block...
NSC319726 is a p53(R175) mutant reactivator, exhibits growth inhibition in cells expressing mutant p53, with IC50 of 8 nM for p53(R175) mutant, shows no inhibit...
Pifithrin-β is a potent p53 inhibitor (IC50=23 uM) in an antiproliferative, showing a conformation similar to those of the prototypical AhR ligand β-naphthoflav...
RO5045337, also known as R7112, RG7112, is a MDM2 antagonist with potential antineoplastic activity. RO5045337 binds to MDM2, thereby preventing the binding of...
NSC59984 is a p53 pathway activator via induction of mutant p53 protein degradation and p73 activation.
MX69 inhibits expression of both MDM2 and XIAP, used for cancer treatment. MX69 blocks the MDM2 protein-XIAP RNA interaction, leading to MDM2 degradation.
RITA (NSC 652287)
NVP-HDM201 (HDM201) is a potent and highly specific MDM-2/p53 inhibitor that binds to human Mdm2 protein with a sub-nanomolar Ki value, activates p53 and induce...
Kevetrin hydrochloride is a water-soluble small molecule with potential antineoplastic activity.
YH239-EE inhibits the growth of OCI-AML-3 cells with wild type p53 by inhibiting the p53-MDM2 interaction.
Serdemetan, also known as JNJ-26854165, is an orally bioavailable, small-molecule HDM2 antagonist with potential antineoplastic activity. HDM2 antagonist JNJ-2...
MI-773, a spirooxindole derivative, is a MDM2 antagonist that has probable effect in the treatment of sorts of cancers. It has already discontinued the Phase I ...
Nutlin-3b, the active enantiomer of Nutlin-3, inhibits the p53/MDM2 interaction with IC50 of 90 nM.
Pifithrin-α is an inhibitor of p53, inhibiting p53-dependent transactivation of p53-responsive genes.
RO8994, a spiroindolinone derivative, is an effective MDM2 inhibitor and has been found to have prabable activity against haematological malignancies. IC50: 5 n...
Pifithrin-β hydrobromide is a reversible inhibitor of p53-dependent transcription and apoptosis, inhibits the growth of the cancer cell lines IGROV-1 (IC50 = 23...