CBL0137

Description: CBL0137 (Curaxin 137), a metabolically stable curaxin, activates p53 (EC50: 0.37 µM) and inhibits NF-kappaB (EC50: 0.47 µM). It functionally inactivates the facilitates chromatin transcription complex (FACT), driving the effects on p53 and NF-kappaB and promoting cancer cell death. CBL0137 has broad anticancer activity in mice when administered orally, eradicates drug-resistant cancer stem cells, and potentiates the efficacy of gemcitabine in preClinicalal models of pancreatic cancer. Target: NF-kappaB, p53. Smiles: C(CNC(C)C)N1C=2C(C=3C1=CC=C(C(C)=O)C3)=CC(C(C)=O)=CC2. References: Gasparian, AV. et al. Curaxins: Anticancer compounds that simultaneously suppress NF-kappaB and activate p53 by targeting FACT. Sci.Transl.Med. 3(95), (2011).