BCI-024

BCI-024 is a small molecule inhibitor of Dual Specificity Phosphatase 1 (DUSP1), also known as Mitogen-Activated Protein Kinase Phosphatase 1 (MKP-1). DUSP1 is a member of the dual-specificity phosphatase family that negatively regulates the mitogen-activated protein kinase (MAPK) signaling pathways by dephosphorylating threonine and tyrosine residues on p38 and c-Jun N-terminal kinase (JNK). In many human cancers, including various adenocarcinomas, DUSP1 is overexpressed and acts as a survival factor by suppressing pro-apoptotic stress signaling and contributing to chemoresistance. BCI-024 was identified as a potent inhibitor that blocks DUSP1 activity, thereby sustaining the phosphorylation of p38 and JNK, which sensitizes tumor cells to DNA-damaging agents and promotes programmed cell death. Developed primarily in an academic setting at the University of Pittsburgh, BCI-024 serves as a chemical probe and a potential therapeutic lead for targeting the MAPK phosphatase family in oncology.

Brand names

Buspirone HCl Tablets

Other names

BCI24BCI-24BCI 24