KC01 is an effective and selective inhibitor of ABHD16A. By measuring competitive gel-based ABPP (IC50 values of inhibition of ABHD16A by KC01 and KC02: ~0.2–0.5 μM and >10 μM, respectively). Testing by a PS substrate assay, IC50 values of inhibition of h

KC01 can deplete lysoPSs from cells, including lymphoblasts derived from subjects with PHARC. It was shown that KC01, but not KC02, inhibited the PS lipase activity of brain membrane lysates from 2-month-old Abhd12+/+ and Abhd12?/? mice. K562 cell lines were treated with varying concentrations of KC01 for 4 h and analyzed the cell membrane fractions by gel-based ABPP, which confirmed in situ inhibition of ABHD16A (IC50: ~ 0.3 μM). In mouse macrophages, disruption of ABHD12 and ABHD16A increases and decreases both lyso-PSs and lipopolysaccharide-induced cytokine production. Knockout mice of Abhd16a?/? have decreased brain lyso-PSs, which runs counter to the elevation in lyso-PS.