MDM2
The murine double minute 2 (MDM2) is a protein encoded by the mdm2 gene that functions as an E3 ubiquitin ligase to ubiquitinate the p53 tumor suppressor and promotes the proteasomal degradation of p53. Human MDM2 protein is a phosphoprotein of 491 amino acids that inherits the E3 ubiquitin ligase activity from its evolutionarily conserved COOH terminal of RING finger domain (Zinc-binding), a common motif in E3 ligases. Human MDM2 protein mediates monomeric ubiquitination on multiple lysine residues mainly in the COOH terminus of p53 and directly inhibits the transcriptional activity of p53 through binding to the NH2 terminal transactivation domain of p53.
- A4209 NSC 207895 (XI-006)Target: MDMXSummary: MDMX inhibitor,anti-cancer agent
- A4230 NSC 66811Summary: MDM2 inhibitor
- A4204 JNJ-26854165 (Serdemetan)1 CitationTarget: p53|HDM2 ubiquitin ligaseSummary: P53 activator, blocking Mdm2-p53 interaction
- A4202 RITA (NSC 652287)Summary: Mdm2-p53 interaction and p53 ubiquitination blocking
- A3762 RG71125 CitationTarget: MDM2Summary: MDM2 inhibitor, first clinical
- A3763 RG73882 CitationSummary: MDM2 antagonist, oral, selective
- B4756 YH239-EESummary: p53-MDM2 antagonist, potent
- B4813 Pifithrin-βSummary: potent p53 inhibitor
- B4984 MI-77301 (SAR405838)Summary: orally available MDM2 antagonist
- B6058 (±)-Nutlin-3Summary: MDM2 antagonist, potent and selective