HA130 is a selective autotaxin (ATX) inhibitor with an IC50 of 28 nM.
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].
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].
References:
[1]. Zhang Y, et al. Autotaxin through lysophosphatidic acid stimulates polarization, motility, and transendothelial migration of naive T cells. J Immunol. 2012 Oct 15;189(8):3914-3924.
[2]. Bai Z, et al. Constitutive lymphocyte transmigration across the basal lamina of high endothelial venules is regulated by theautotaxin/lysophosphatidic acid axis. J Immunol. 2013 Mar 1;190(5):2036-2048.