Fig. 1: DF-003 is a potent and selective inhibitor of ALPK1.
From: Discovery of a selective alpha-kinase 1 inhibitor for the rare genetic disease ROSAH syndrome
a Chemical structure of DF-003. b An in vitro kinase assay was performed using recombinant human ALPK1, human TIFA, and ADP-D-heptose in a kinase reaction buffer containing 3-fold dilutions of DF-003. After adding [33P]-ATP, the kinase reaction was allowed to proceed at room temperature for 60 min, after which ALPK1 kinase activity was quantified and expressed as the percentage of remaining ALPK1 kinase activity relative to vehicle (DMSO, no DF-003) conditions. Each condition was measured without replication but the assay was conducted 4 times with similar results. c The top 3 non-ALPK1 human kinases against which DF-003 was found to exhibit the most potent inhibitory activity in an in vitro kinase assay-based screen of 394 human kinases are presented with calculated DF-003 IC50 values.
