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APR-246 (Eprenetapopt) is the first-in-class small molecule to restore wild-type p53 function in TP53 mutant cells.
APR-246 (Eprenetapopt), also known as PRIMA-1MET, is a quinuclidinone derivative that targets the Wrap53 gene with potential antineoplastic activity. APR-246 (PRIMA-1MET) enhances apoptosis in mutant p53 carrying cells, compared to the p53 null parental cells. Most p53 mutants are in complex with Hsp70 proteins. APR-246 treatment increases Hsp70 expression and nucleolar translocation, in parallel with the induction of nucleolar accumulation of mutant p53. Several lines of evidence suggest that APR-246 can also act independently of the p53 status of the cell. APR-246 (Eprenetapopt) is the first small molecule to restore wild-type p53 function in TP53 mutant cells. APR-246 also targets the selenoprotein thioredoxin reductase 1 (TrxR1), a key regulator of REDOX balance in cells.
In animal studies, APR-246 (Eprenetapopt) is well tolerated, APR-246 single treatment inhibits tumor growth by 21% in mice bearing the aggressively growing A2780-CP20 tumor xenografts.
| Molecular Weight | 199.25 |
| Formula | C10H17NO3 |
| CAS Number | 5291-32-7 |
| Solubility (25°C) | DMSO ≥ 60 mg/mL Water ≥ 40 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. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
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