1017606-66-4

LPA₂ antagonist 1 is an antagonist of lysophosphatidic acid receptor 2 (LPA₂; IC₅₀ = 17 nM). 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.

N-[(2S)-1-[4-(3,4-Dichlorophenyl)sulfonylpiperazin-1-yl]propan-2-yl]-7-methylthieno[3,2-d]pyrimidin-4-amine is a Lpa2 protein antagonists.

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[1] HILARY P. BECK . Discovery of potent LPA2 (EDG4) antagonists as potential anticancer agents[J]. Bioorganic & Medicinal Chemistry Letters, 2008, 18 3: Pages 1037-1041. DOI: 10.1016/j.bmcl.2007.12.024