LPA2 antagonist 2 (H2L 5226501) is a selective LPA₂ antagonist with an IC₅₀ of 28.3 nM and a K_i of 21.1 nM. LPA2 antagonist 2 is ＞480-fold more selective than LPA₃ (IC₅₀ of 13.85 μM)^[1]. IC50 & Target: IC50: 28.3 nM (LPA₂); 13.85 μM (LPA₃)^[1] In Vitro: Lysophosphatidic acid (LPA) is a phospholipid mediator that elicits a host of biological effects including cell proliferation, survival, motility and differentiation. LPA has been shown to regulate cancer cell invasion, metastasis, and resistance to both chemotherapeutics and radiation. LPA2 antagonist 2 (H2L 5226501) inhibits LPA₁ with an Imax of 59.0% at 30 µM^[1].