AGPAT4-IN-1

AGPAT4-IN-1 (Compound CL26) is a covalent AGPAT4 inhibitor with an IC50 of 795 nM. AGPAT4-IN-1 covalently binds to AGPAT4 at Cys228 and significantly inhibits acyltransferase activity, LPA-to-PA conversion and downstream mTOR/S6K pathways. AGPAT4-IN-1 sensitizes hepatocellular carcinoma (HCC) tumors to Sorafenib (HY-10201) and significantly induces apoptosis with a synergistic response. AGPAT4-IN-1 has antitumor activity and reduces tumorigenicity and stemness in HCC xenograft mouse models[1].

Product Specifications

CAS Number

[2411250-59-2]

UNSPSC

12352100

Target

Acyltransferase; Apoptosis; mTOR; Ribosomal S6 Kinase (RSK)

Related Pathways

Apoptosis; MAPK/ERK Pathway; Metabolic Enzyme/Protease; PI3K/Akt/mTOR

Field of Research

Cancer

Smiles

O=C(CCl)NCC(O1)=CC=C1C(S2)=NC3=C2C=CC=C3

Molecular Formula

C14H11ClN2O2S

Molecular Weight

306.77

References & Citations

[1]Ng KY, et al. AGPAT4 targeted covalent inhibitor potentiates targeted therapy to overcome cancer cell plasticity in hepatocellular carcinoma mouse models. Sci Transl Med. 2025 Jul 30;17 (809) :eadn9472.