CEP1347

CEP1347 (also known as KT7515) is an orally active, semisynthetic small molecule derivative of the indolocarbazole K-252a. It functions as a potent and selective inhibitor of the mixed lineage kinase (MLK) family, with high affinity for MAP3K11 (MLK3), MAP3K9 (MLK1), and MAP3K10 (MLK2). By inhibiting these kinases, CEP1347 prevents the activation of the c-Jun N-terminal kinase (JNK) signaling pathway, which is a critical mediator of programmed cell death (apoptosis) in neurons under stress. Developed by Cephalon, the compound was primarily investigated for its neuroprotective effects in Parkinson's disease. It reached Phase 2/3 clinical testing in the PRECEPT trial, which aimed to delay the need for dopaminergic therapy in early-stage patients; however, the trial was terminated early due to a lack of efficacy. Beyond neurodegeneration, CEP1347 has been explored in preclinical and early clinical research for its potential to target cancer stem cells in various malignancies, including glioblastoma and pancreatic cancer.

Other names

156177-65-0