HTS01037

HTS01037 is a small-molecule inhibitor primarily characterized as a high-affinity competitive antagonist of adipocyte fatty acid-binding protein 4 (FABP4, also known as AFABP/aP2), with a Ki of approximately 0.67 μM. Mechanistically, HTS01037 antagonizes FABP4-mediated protein-protein interactions and interferes with fatty acid binding. In preclinical studies, HTS01037 has demonstrated anticancer activity (notably in pancreatic ductal adenocarcinoma models) by inhibiting cellular proliferation, epithelial-mesenchymal transition (EMT), and cancer stemness, and by inducing apoptosis. Additionally, HTS01037 suppresses lipolysis in adipocytes and reduces inflammation in macrophages. The compound has also shown efficacy in models of inflammation and neoplastic disease, indicating translational potential for cancer (notably PDAC) and metabolic/inflammatory disorders. HTS01037 does not activate peroxisome proliferator-activated receptor γ (PPARγ)[1][2][3][4][5][6][7][9].

Other names

HTS01037HTS-01037HTS 010371