FC-114

FC-114 is a small molecule inhibitor of Protein Tyrosine Phosphatase 1B (PTP1B), chemically characterized as an indole-fused derivative of glycyrrhetinic acid. PTP1B is a critical enzyme that negatively regulates insulin and leptin signaling pathways, making it a significant target for metabolic diseases. FC-114 has demonstrated potent inhibitory activity against PTP1B in vitro and has been shown to enhance the mRNA expression of the GLUT4 receptor in C2C12 myoblast cells. In preclinical studies using streptozotocin-induced diabetic mice, FC-114 and its amino acid conjugates (such as those with glycine and serine) significantly reduced blood glucose levels and improved insulin tolerance. The mechanism of action is consistent with uncompetitive inhibition, potentially involving binding to the disordered C-terminal domain of the PTP1B enzyme.

Other names

indole-fused glycyrrhetinic acid derivative