TC LPA₅ 4

TC LPA₅ 4 is an antagonist of lysophosphatidic acid receptor 5 (LPA₅; IC₅₀ = 0.8 µM in McA-RH7777 cells expressing the human receptor).¹ It selectively inhibits the aggregation of washed isolated human platelets induced by 16:0 alkyl-LPA (1-palmitoyl LPA; Item Nos. 10010094 | 10010290) over collagen or thrombin receptor activating peptide (TRAP; IC₅₀s = 0.8, >10, and >10 µM, respectively). TC LPA₅ 4 also inhibits the histone-lysine N-methyltransferase NSD2 (IC₅₀ = 8.5 µM) and 29 other methyltransferases (IC₅₀s = 0.33-71 µM).² It reduces tumor volume in a CGTH-W-3 thyroid cancer mouse xenograft model when administered at a dose of 10 mg/kg.³ TC LPA₅ 4 (10 mg/kg, i.p.) prevents brain tissue loss and neurological deficits, as well as increases survival, neurogenesis in the subventricular zone, and angiogenesis in the penumbra, in a mouse model of ischemic stroke induced by transient middle cerebral artery occlusion (MCAO).⁴

WARNING This product is not for human or veterinary use.

1. Kozian, D.H., Evers, A., Florian, P., et al. Selective non-lipid modulator of LPA₅ activity in human platelets. Bioorg. Med. Chem. Lett. 22(16), 5239-5243 (2012).

2. Coussens, N.P., Kales, S.C., Henderson, M.J., et al. High-throughput screening with nucleosome substrate identifies small-molecule inhibitors of the human histone lysine methyltransferase NSD2. The Journal of Biological Chemisty 293(35), 13750-13765 (2018).

3. Zhao, W.-J., Zhu, L.-L., Yang, W.-Q., et al. LPAR5 promotes thyroid carcinoma cell proliferation and migration by activating class IA PI3K catalytic subunit p110β. Cancer Sci. 112(4), 1624-1632 (2021).

4. Sapkota, A., Park, S.J., and Choi, J.W. Inhibition of LPA₅ activity provides long-term neuroprotection in mice with brain ischemic stroke. Biomol. Ther. (Seoul) 28(6), 512-518 (2020).