cbl0137

CBL0137 is a small molecule anticancer agent belonging to the curaxin class. It acts primarily by targeting and inhibiting the Facilitates Chromatin Transcription (FACT) complex, a histone chaperone involved in chromatin remodeling and gene transcription. By binding to FACT and sequestering it on chromatin, CBL0137 inhibits its activity, which disrupts the transcription of genes critical for cancer cell survival—including those regulated by NF-κB and heat shock transcription factor 1 (HSF1)—and simultaneously activates p53 tumor suppressor pathways. This multi-modal mechanism results in antineoplastic effects such as inhibition of cell proliferation and induction of apoptosis in cancer cells. CBL0137 is being developed for use against relapsed or refractory solid tumors (including central nervous system tumors), lymphoma, hematological malignancies, pancreatic ductal adenocarcinoma, melanoma, sarcoma, osteosarcoma, diffuse intrinsic pontine glioma (DIPG), and other diffuse midline gliomas[2][4][5][6][8][9].

Other names

curaxin cbl0137