cc-401

Description: CC-401 is a potent, specific, second generation and ATP-competitive anthrapyrazolone c-Jun N terminal kinase (JNK) inhibitor with potential antineoplastic activity. It is a potent inhibitor of all three forms of JNK with Ki of ranging from 25 to 50 nM. It inhibits sorbitol-induced phosphorylation of c-Jun in a dosage-dependent manner. However, CC-401 does not prevent sorbitol-induced phosphorylation of JNK, p38, or ERK. The specific JNK inhibitor, CC-401, was synthesized by Celgene Corporation as a competitive inhibitor of the ATP binding site in the active, phosphorylated form of JNK. CC-401 has at least 40-fold selectivity for JNK compared with other related kinases. However, the phase 1 clinical trials (NCT00126893) of CC-401 for Myeloid Leukemia was terminated.

References: J Am Soc Nephrol. 2007 Feb; 18(2):472-84; Cell Syst. 2018 Apr 25; 6(4):424-443.e7.

Related CAS#: 1438391-30-0 (HCl)