AGPAT4-IN-1

AGPAT4-IN-1 (Compound CL26) is a covalent AGPAT4 inhibitor with an IC50 of 795 nM. It binds covalently to the Cys228 site of AGPAT4, significantly inhibiting acyltransferase activity, the conversion of LPA to PA, and the downstream mTOR/S6K pathway. AGPAT4-IN-1 enhances the sensitivity of hepatocellular carcinoma (HCC) tumors to Sorafenib and significantly induces apoptosis through synergistic effects. This compound exhibits antitumor activity and reduces tumorigenicity and stem cell characteristics in a hepatocellular carcinoma xenograft mouse model.