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SCH529074

Catalog No. T37042   CAS 922150-11-6
Synonyms: SCH 529074

SCH529074 is a selective activator of p53 (Ki = 1 μM) and can be used in studies about non-small-cell lung carcinoma. SCH529074 restores mutant p53 function and interrupts HDM2-mediated ubiquitination of wild Type p53.

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SCH529074 Chemical Structure
SCH529074, CAS 922150-11-6
Pack Size Availability Price/USD Quantity
1 mg In stock $ 44.00
2 mg In stock $ 64.00
5 mg In stock $ 97.00
10 mg In stock $ 178.00
25 mg In stock $ 387.00
50 mg In stock $ 576.00
100 mg In stock $ 823.00
1 mL * 10 mM (in DMSO) In stock $ 116.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description SCH529074 is a selective activator of p53 (Ki = 1 μM) and can be used in studies about non-small-cell lung carcinoma. SCH529074 restores mutant p53 function and interrupts HDM2-mediated ubiquitination of wild Type p53.
Targets&IC50 p53 DBD:1-2 μM (Ki)
In vitro SCH529074 (2-4 µM) reduces cell viability and decreases to 20-25% in p53 mutant cells including H157, H1975, and H322, and to 68% in the p53 WT cell line A549 at 4 µM. SCH 529074 (2-4 µM) induces NSCLC cells including H157, A549, HCT116, and HCT116 p53-/- arrested at the G0/G1 phase (59%; 72%; 66%; and 57%)[2].
In vivo In female nude mice, 5–7 weeks of age, received subcutaneous inoculation of DLD-1 human colorectal carcinoma cells, SCH529074 (orally; 30 and 50 mg/kg) reduces 79 and 43% of tumor growth with the plasma exposure of 0.26–0.55 μm at 30 mg/kg and 0.39-0.79 μm at 50 mg/kg[1].
Synonyms SCH 529074
Molecular Weight 563.56
Formula C31H36Cl2N6
CAS No. 922150-11-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 33 mg/mL

DMF: 33 mg/mL

DMSO: 22.5mg/mL (39.9mM)

TargetMolReferences and Literature

1. Demma, M., Maxwell, E., Ramos, R., et al. SCH529074, a small molecule 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. J. Biol. Chem. 285(14), 10198-10212 (2010). 2. Miljana Nenkov, et al. Growth Inhibitory Role of the p53 Activator SCH 529074 in non‑small Cell Lung Cancer Cells Expressing Mutant p53. Oncol Rep. 2020 Jun;43(6):2073-2082.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Active Compound Library Anti-Lung Cancer Compound Library Bioactive Compounds Library Max Anti-Cancer Metabolism Compound Library Anti-Cancer Compound Library Anti-Pancreatic Cancer Compound Library Bioactive Compound Library

Related Products

Related compounds with same targets
Phenoxodiol CBL0137 DPBQ Verbascoside ZMC1 Isoliquiritin p53-MDM2-IN-1 ReACp53 acetate

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Keywords

SCH529074 922150-11-6 Apoptosis p53 SCH-529074 SCH 529074 inhibitor inhibit

 

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