||BH3I-1 is a Bcl-2 antagonist.
||RITA(NSC 652287) induced cross-links of both DNA-DNA and DNA-protein with no detectable DNA single-strand breaks. RITA, like nutlin-3, can disrupt the p53/Mdm2 interaction.
||Tenovin-1 inhibits protein-deacetylating activities of SirT1 and SirT2 and protects against MDM2-mediated p53 degradation, which involves ubiquitination.
||Nutlin-3 is an MDM2 antagonist. Nutlin-3 inhibits the MDM2-p53 interaction (IC50: 0.09 μM) and activates p53. Antiproliferative agent; chemotherapeutic agent; induces apoptosis in Y cells.
||Triptolide is a diterpenes trioxide, immunosuppressive agent extracted from the Chinese herb Tripterygium wilfordii.
||Serdemetan is an orally bioavailable HDM2 antagonist with potential antineoplastic activity.
||Kevetrin hydrochloride is a small molecule and activator of the tumor suppressor protein p53, with potential antineoplastic activity.
||RO8994 is a highly effective and specific inhibitor of spiroindolinone small-molecule MDM2, with IC50 of 20 nM (MTT proliferation assays) and 5 nM (HTRF binding assays).
||MX69 is the MDM2/XIAP inhibitor, blocking the MDM2 protein-XIAP RNA interaction, leading to MDM2 degradation.
||Nutlin-3a, the active enantiomer of Nutlin-3, inhibits MDM2-p53 interactions and stabilizes the p53 protein.
||YH239-EE, the ethyl ester of YH239, is a potent p53-MDM2 antagonist and an apoptosis inducer.
||Idasanutlin (RG-7388) is an effective and specific p53-MDM2 inhibitor (IC50: 6 nM).
||MI-773 (SAR405838) is an orally available MDM2 antagonist with Ki of 0.88 nM. Phase 1.
||NSC 207895 suppresses MDMX with IC50 of 2.5 μM, leading to enhanced p53 stabilization/activation and DNA damage, and also regulates MDM2, an E3 ligase.
||Nutlin-3b is a p53/MDM2 antagonist or inhibitor (IC50: 13.6 μM), 150-fold less potent (+)-enantiomer of Nutlin-3 as in comparison with opposite (-)-enantiomer Nutlin-3a.
||RG7112 (RO5045337) is an orally bioavailable and selective p53-MDM2 inhibitor.