TSI-01

TSI-01 is a selective LPCAT2 inhibitor, with IC₅₀ values of 0.47 μM and 3.02 μM against LPCAT2 and LPCAT1, respectively. TSI-01 competitively inhibits acetyl-CoA (acetyl-CoA) targeting the lysophosphatidic acid acetyltransferase activity of LPCAT2, and suppresses PAF biosynthesis in calcium ionophore-stimulated mouse peritoneal macrophages. TSI-01 inhibits the proliferation of endometrial cancer cells and promotes endometrial cancer cell apoptosis (apoptosis). TSI-01 can be used for the research of endometrial cancer and PAF-related inflammatory diseases^[1][2]. In Vitro:TSI-01 (0-40 μM) potently inhibits the viability of human endometrial cancer Ishikawa cells with an IC₅₀ of 7.56 μM and HEC-1A cells with an IC₅₀ of 9.31 μM^[1].
TSI-01 (0-10 μM) concentration-dependently promotes apoptosis in human endometrial cancer Ishikawa and HEC-1A cells, with 10 μM inducing the highest levels of early and late apoptosis^[1].
TSI-01 (0.1-100 μM; 1 h) dose-dependently inhibits A23187-induced PAF production in RAW-mLPCAT2 cells with an IC₅₀ of 38.8 μM, without reducing cell viability^[2].