DF-003

DF-003 is a selective, orally active, ATP-competitive ALPK1 inhibitor capable of crossing the blood-brain barrier. It effectively inhibits human ALPK1 and ALPK1[T237M] with IC50 values of 1.5 nM and 16 nM, respectively. The compound exhibits selectivity over the nearest kinase by more than 860-fold. DF-003 suppresses the upregulation of TNF, CXCL10, or CXCL8 in HEK-293 cells. It has applications in the study of retinopathy, optic nerve edema, splenomegaly, anhidrosis, and headaches associated with ROSAH syndrome.