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CBL0137 is a metabolically stable curaxin that activates p53 with an EC50 value of 0.37 µM and inhibits NF-κB with an EC50 of 0.47 µM. CBL0137 inhibits histone chaperone FACT, is efficacious in preclinical orthotopic models of temozolomide-responsive and -resistant glioblastoma. CBL0137 eradicates d rug resistant cancer stem cells and potentiates efficacy of gemcitabine in preclinical models of pancreatic cancer.
In mice, CBL0137 was effective against orthotopic gemcitabine resistant PANC-1 model and patient derived xenografts, in which CBL0137 anti-tumor effect related with overexpression of FACT. Moreover, the combination effects of CBL0137 and gemcitabine might be explained by the ability of CBL0137 to inhibit several transcriptional programs induced by gemcitabine, including NF-kappaB response and expression of ribonucleotide reductase.
| Molecular Weight | 336.43 |
| Formula | C21H24N2O2 |
| CAS Number | 1197996-80-7 |
| Solubility (25°C) | DMSO 10 mM |
| 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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