HA130 is a selective autotaxin (ATX) inhibitor with an IC₅₀ of 28 nM. In Vitro: HA130 completely blocks the ability of ATX to promote TEM (transendothelial migration). HA130 at 0.3 μM completely ablates the activity of ATX on TK1 uropod formation^[1]. In Vivo: HA130 slows T cell migration across lymph node HEVs. HA130 decreases the "outside HEVs/inside HEVs" ratio by 3-4-fold compared to vehicle-treated animals vehicle^[1].
The s.c. administration of HA130 induces marked lymphocyte accumulation within the endothelial cell (EC) and sub-EC layers of HEVs in draining lymph nodes (LNs)^[2].