cbl0137

Description: CBL0137 (formerly known as Curaxin 137 or CBL-0137) is an inhibitor of the histone chaperone, FACT (facilitates chromatin transcription complex). It also activates p53 and inhibits NF-kB with EC50s of 0.37 uM and 0.47 uM in the cell-based p53 and NF-kB reporter assays, respectively. CBL0137 has entered clinical trials for Glioblastoma and Hematological Malignancies. CBL0137 eradicates drug resistant cancer stem cells and potentiates efficacy of gemcitabine in preclinical models of pancreatic cancer. Curaxins modulate several important signaling pathways involved in the pathogenesis of Pancreatic ductal adenocarcinoma (PDA) through inhibition of chromatin remodeling complex FACT. FACT is overexpressed in multiple types of tumor, with one of the highest rate of overexpression in PDA (59%).

References: Oncotarget. 2014 Nov 30; 5(22):11038-53; Sci Transl Med. 2011 Aug 10; 3(95):95ra74.