Chemical Name: 2-[[3-(1,3-dioxo-1H-benz[de]isoquinolin-2(3H)-yl)propyl]thio]benzoic acid
Biological ActivityGRI 977143 is a selective lysophosphatidic acid 2 (LPA2) receptor non-lipid agonist (EC50 = 3.3 μM). Does not activate other LPA GPCRs at concentrations up to 10 μM. Antiapoptotic; inhibits activation of caspases 3, 7, 8 and 9, Bax translocation and PARP-1 cleavage. Activates ERK1/2 survival pathway.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Virtual screening for LPA2-specific agonists identifies a nonlipid compound with antiapoptotic actions.
Kiss et al.
Mitigation of radiation injury by selective stimulation of the LPA(2) receptor.
Kiss et al.
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