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LPA2 antagonist 1 is an antagonist of lysophosphatidic acid receptor 2 (LPA2; IC50 = 17 nM).1 It is selective for LPA2 over LPA1 and LPA3 (IC50s = >50 μM). LPA2 antagonist 1 inhibits HGF-induced phosphorylation of ERK and proliferation of HCT116 colon cancer cells in a concentration-dependent manner.
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1. Discovery of potent LPA2 (EDG4) antagonists as potential anticancer agents. Bioorg. Med. Chem. Lett. 18(3), 1037-1041 (2008).