JNJ-26854165

The E3 ubiquitin ligase known as murine double minute 2 (MDM2, HDM2 in humans) binds to and then ubiquitinates several proteins, most notably the tumor suppressor p53. JNJ-26854165 is an antagonist of MDM2 that suppresses the growth of cancer cell lines expressing wild-type p53 (IC50 values range from 240-440 nM). It induces p53-mediated transcription culminating in apoptotic death of acute leukemia cells. JNJ-26854165 is orally bioavailable and has anti-proliferative as well as apoptotic actions in various tumor models. As MDM2 interacts with and modulates several targets in addition to p53, JNJ-26854165 affects multiple signaling pathways.Formal Name: N1-[2-(1H-indol-3-yl)ethyl]-N4-4-pyridinyl-1,4-benzenediamine. CAS Number: 881202-45-5. Synonyms: Serdemetan. Molecular Formula: C21H20N4. Formula Weight: 328.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 25 mg/ml, DMF:PBS (pH 7.2) (1:5): 0.1 mg/ml, DMSO: 20 mg/ml, Ethanol: 1 mg/ml. lambdamax: 223, 284 nm. SMILES: C1(NC2=CC=C(NCCC3=CNC4=C3C=CC=C4)C=C2)=CC=NC=C1. InChi Code: InChI=1S/C21H20N4/c1-2-4-21-20(3-1)16(15-24-21)9-14-23-17-5-7-18(8-6-17)25-19-10-12-22-13-11-19/h1-8,10-13,15,23-24H,9,14H2,(H,22,25). InChi Key: CEGSUKYESLWKJP-UHFFFAOYSA-N.