CBL0137 (hydrochloride) Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
Curaxins are small molecules that simultaneously activate p53 and inhibit NF-κB without causing detectable genotoxicity. CBL0137 is a water soluble and metabolically stable curaxin that activates p53 with an EC
50 value of 0.37 μM and inhibits NF-κB with an EC
50 value of 0.47 μM. It functionally inactivates the facilitates chromatin transcription complex, driving the effects on p53 and NF-κB and promoting cancer cell death. CBL0137 has broad anticancer activity in mice when administered orally, eradicates drug-resistant cancer stem cells, and potentiates efficacy of gemcitabine in preclinical models of pancreatic cancer.
Verwenden
Curaxins are small molecules that simultaneously activate p53 and inhibit NF-κB without causing detectable genotoxicity. CBL0137 is a water soluble and metabolically stable curaxin that activates p53 with an EC50 value of 0.37 μM and inhibits NF-κB with an EC50 value of 0.47 μM. It functionally inactivates the facilitates chromatin transcription complex, driving the effects on p53 and NF-κB and promoting cancer cell death. CBL0137 has broad anticancer activity in mice when administered orally, eradicates drug-resistant cancer stem cells, and potentiates efficacy of gemcitabine in preclinical models of pancreatic cancer.[Cayman Chemical]
Biologische Aktivit?t
CBL0137 (CBLC137, Curaxin 137) HCl activates p53 and inhibits NF-kB with IC50 of 0.37 μM and 0.47 μM, respectively, in cell experiments. It also inhibits the histone molecular chaperone FACT, which promotes the formation of chromatin transcriptional complexes.
CBL0137 (hydrochloride) Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
