325850-81-5

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. 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-[3-(1,3-Dioxo-1H,3H-benzo[de]isoquinolin-2-yl)-propylsulfanyl]-benzoic acid is used as a non-lipid agonist of LPA2. LPA (Lipoprotein Associated Phospholipase A2/A3 are important factors in prediction of diseases involving fatty acids such as coronary heart disea se or atherosclerosis.

ChEBI: GRI977143 is a benzoisoquinoline that is 1H-benzo[de]isoquinoline-1,3(2H)-dione in which the hydrogen attached to the nitrogen has been replaced by a 3-[(2-carboxyphenyl)thio]propyl group. It is a selective LPA2 receptor non-lipid agonist. It has a role as a G-protein-coupled receptor agonist and an apoptosis inhibitor. It is a benzoisoquinoline, an aryl sulfide and a member of benzoic acids.

LPA₂ Receptor: 3.3 μM (EC₅₀)

Store at +4°C

[1] GY?NGYI N KISS. Virtual screening for LPA2-specific agonists identifies a nonlipid compound with antiapoptotic actions.[J]. Molecular Pharmacology, 2012, 82 6: 1162-1173. DOI: 10.1124/mol.112.079699
[2] GY?NGYI N. KISS . Mitigation of radiation injury by selective stimulation of the LPA2 receptor[J]. Biochimica et biophysica acta. Molecular and cell biology of lipids, 2013, 1831 1: Pages 117-125. DOI: 10.1016/j.bbalip.2012.08.020