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SCH529074 is an orally active, potent activator of mutant p53, which binds p53 DNA binding domain (DBD), restores growth-suppressive function to mutant p53 and interrupts HDM2-mediated ubiquitination of wild type p53. SCH529074 treatment caused significant reduction in cell viability and colony formation activity in p53 mutant, p53 WT and p53‑deficient cells. The treatment of NSCLC cells with SCH529074 resulted in a dose‑dependent induction of apoptosis and G0/G1 cell cycle arrest, which was associated with the activation of caspases (3 and 7), p53‑independent upregulation of p21 and PUMA as well as increased LC3II, a biomarker of autophagy. The combination treatment with the autophagy inhibitor chloroquine (CQ) and SCH529074 led to decreased cell viability, colony formation and increased induction of apoptosis.
| Molecular Weight | 563.56 |
| Formula | C31H36Cl2N6 |
| CAS Number | 922150-11-6 |
| Solubility (25°C) | DMSO 20 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related p53 Products |
|---|
| Pifithrin-α, p-Nitro, Cyclic
Pifithrin-α, p-Nitro, Cyclic (PFN-α) is cell-permeable and active-form p53 inhibitor. Pifithrin-α, p-Nitro, Cyclic behaves as a p53 posttranscriptional activity inhibitor. Pifithrin-α, p-Nitro, Cyclic do not prevent p53 phosphorylation on the S15 residue. |
| PK095
PK095 is a p53 mutant stabilizer. |
| HLI373
HLI373 is an efficacious Hdm2 inhibitor. |
| Cjoc42
Cjoc42 is a compound capable of binding to gankyrin. |
| MDM2-IN-1
MDM2-IN-1 is a synthetic MDM2-p53 interaction (MDM2) inhibitor and contains the trans (D-)configuration. |
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Products are for research use only. Not for human use. We do not sell to patients.
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