NSC-59984

SKU: orb1223967

Description

A small molecule that both destabilize mutant p53 and restores wild-type p53 pathway in cancer cells; induces mutant p53 protein degradation via MDM2 and the ubiquitin-proteasome pathway, restores wild-type p53 signaling via p73 activation, specifically in mutant p53-expressing colorectal cancer cells. degrades mutant p53R273H, rescued CDH6 expression; significantly represses DLD-1 xenograft tumor growth.

Key Properties

• CAS Number: 803647-40-7
• MW: 265.2652
• Purity: >98% (HPLC)
• Formula: C₁₂H₁₅N₃O₄
• SMILES: O=C(N1CCN(C)CC1)/C=C/C2=CC=C([N+]([O-])=O)O2
• Target: MDM2-p53
• Solubility: DMSO: ≥ 38 mg/mL

Bioactivity

• In Vivo:
  NSC59984 synergizes with CPT11 to induce cell death in mutant p53-expressing colorectal cancer cells and inhibits mutant p53-associated colon tumor xenograft growth in a p73-dependent manner.
• In Vitro:
  NSC59984 specifically restores p53 pathway signaling in mutant p53-expressing human colorectal cancer cells. NSC59984 induces cell death in tumor cells but not normal cells with little or no genotoxicity. NSC59984 induces mutant p53 protein degradation through MDM2-mediated ubiquitination in cancer cells. NSC59984 restores p53 pathway signaling through activation of p73. NSC59984 induces p73-dependent cell apoptosis in cancer. The EC50 of NSC59984 in most cancer cells is significantly lower than those of normal cells, with EC50 of 8.38 μM for p53-null HCT116 cells.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

NSC 59984 | NSC59984

Quick Database Links

Gene Symbol

MDM2-p53