Autotaxin is a lysophospholipase D, cleaving lysophosphatidylcholine to produce choline and lysophosphatidic acid (LPA). S32826 is a potent and selective inhibitor of autotaxin, inhibiting recombinant autotaxin β with an IC50 of 8.8 nM. It shows similar effectiveness against the three known autotaxin isoforms (α, β, and γ). It has no effect on a variety of receptors and enzymes, with the exceptions of src (IC50 = 6 μM) and phosphatase 1B (IC50 = 15 μM). S32826 inhibits LPA release from adipocytes (IC50 = 90 nM) and reduces plasma autotaxin activity by 57% when used at 5 μM.
