Drug intelligence / Profile preview

SB-505124

Development stage
Preclinical
Lead developer
GSK
Modality
Small Molecules
Administration
Intraperitoneal, Oral
01

Overview

SB-505124 is a **selective small molecule inhibitor** of transforming growth factor-beta (TGF-β) type I receptors, specifically targeting **ALK4, ALK5 (TGF-βRI), and ALK7**[1][4][6][10]. It acts as a **competitive ATP-binding site inhibitor** for these receptors, thereby blocking downstream signaling of TGF-β and activin pathways while sparing bone morphogenetic protein (BMP) signaling. Its molecular structure is based on an imidazole scaffold and it has demonstrated potent selectivity and efficacy in preclinical models for modulating TGF-β dependent biological processes, such as fibrosis, Th17/Treg balance, and stem cell niches. SB-505124 is mainly used as a **research tool** rather than a clinically approved drug and is widely employed in the preclinical assessment of TGF-β pathway inhibition[1][4][6][10].

Other names
2-(5-benzo[1,3]dioxol-5-yl-2-tert-butyl-3H-imidazol-4-yl)-6-methylpyridineSB-505124 hydrochloride hydrateSB505124 hydrochloride hydrateSB 505124 hydrochloride hydrateTGF-beta RI Inhibitor IIICHEMBL226838CHEMBL-226838CHEMBL 226838694433-59-5
02

Targets

TGFBR1ACVR1C (Activin A Receptor Type 1C)ACVR1B (Activin A receptor type IB)

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