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.
