CEP-11004

CEP-11004 (also known as KT-8138) is a small molecule, ATP-competitive inhibitor of the mixed-lineage kinase (MLK) family, specifically targeting MLK1, MLK2, and MLK3. Developed through a collaboration between Kyowa Kirin and Cephalon, CEP-11004 is a semi-synthetic indolocarbazole derivative of the natural product K252a. By inhibiting MLKs, CEP-11004 prevents the downstream activation of the c-Jun N-terminal kinase (JNK) pathway, which plays a key role in stress-induced apoptosis. Preclinical studies have investigated CEP-11004 for its neuroprotective properties in models of Parkinson's disease (such as MPTP-induced neurotoxicity) and its ability to protect mechanosensory hair cells from aminoglycoside-induced ototoxicity. It has also been studied in oncology models for blocking breast cancer cell migration and metastasis.

Other names

bis-isopropylthiomethyl-K-252abis-isopropylthiomethyl-K252abis-isopropylthiomethyl-K 252a