Drug intelligence / Profile preview

AT-56

Development stage
Preclinical
Lead developer
Shandong University
Modality
Small Molecules
Administration
Oral
01

Overview

AT-56 is a potent, selective, and orally active small molecule inhibitor of lipocalin-type prostaglandin D synthase (L-PGDS, also known as PTGDS). It competitively inhibits L-PGDS by occupying its catalytic pocket, thereby blocking the conversion of prostaglandin H2 (PGH2) to prostaglandin D2 (PGD2). Originally identified by researchers at the Osaka Bioscience Institute, AT-56 has been widely used as a chemical tool to study the role of L-PGDS in various physiological and pathological processes, including sleep regulation, pain, and inflammation. Preclinical research, particularly at Shandong University, has also investigated AT-56 as a potential therapeutic strategy for hematological malignancies, demonstrating that it inhibits cell proliferation, induces cell cycle arrest, and promotes ferroptosis in diffuse large B-cell lymphoma (DLBCL) and peripheral T-cell lymphoma (PTCL) models.

Other names
1-(4-(2H-tetrazol-5-yl)butyl)-4-(5H-dibenzo[a,d][7]annulen-5-ylidene)piperidine4-dibenzo[a,d]cyclohepten-5-ylidene-1-[4-(2H-tetrazol-5-yl)-butyl]-piperidine
02

Targets

PTGDS (Prostaglandin D2 synthase)

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