GRI 977143 is a potent, specific and nonlipid agonist of LPA2 receptor with EC50 of 3.3 uM, does not activate any of the other LPA GPCRs (>10 uM).
GRI 977143 also inhibits LPA3 with IC50 of 6.6 uM.
GRI 977143 reduces the activation of caspases 3, 7, 8 and 9 and inhibits PARP1 cleavage and DNA fragmentation in different extrinsic and intrinsic models of apoptosis in vitro.
GRI 977143 promotes carcinoma cell invasion of human umbilical vein endothelial cell monolayers and fibroblast proliferation.
