GRI-977143 is an agonist of G protein-coupled lysophosphatidic acid receptor 2 (LPA2) with an EC50 value of 3.3 μM in LPA2-transfected RH7777 cells.[1] It is selective for LPA2, having no activity at LPA1, LPA3, LPA4, and LPA5 at concentrations up to 10 μM. GRI-977143 increases growth and reduces caspase-3 and -7 activation in LPA2-transduced MEF fibroblasts. It increases MM1 rat hepatoma cell invasion and inhibits apoptosis of IEC-6 cells induced by TNF-α, doxorubicin, or serum withdrawal. GRI-977143 also rescues apoptotic cells from γ-irradiation-induced injury in vitro and in vivo.[2]