Drug intelligence / Profile preview

SB431542

Development stage
Preclinical
Lead developer
GSK
Modality
Small Molecules
Administration
In Vitro, Intraperitoneal (in Animal Studies)
01

Overview

SB431542 is a potent and selective small molecule inhibitor of activin receptor-like kinase (ALK) family type I receptors—specifically ALK4, ALK5 (also known as TGFβ type I receptor), and ALK7—with an IC50 of 94 nM for ALK5. It acts by competitively binding the ATP-binding site of these serine/threonine kinases, blocking downstream TGF-β and activin signaling. This effectively inhibits phosphorylation of Smad2/3 and subsequent gene regulation mediated by TGF-β family ligands. SB431542 does not inhibit other ALKs that mediate bone morphogenetic protein (BMP) signaling and does not affect MAP kinase (ERK, JNK, p38) pathways. It is widely used in biomedical research to study TGF-β signaling, tissue fibrosis, EMT (epithelial–mesenchymal transition), tumor progression, stem cell maintenance, and differentiation[1][2][4][7][8][9][10].

Other names
4-(4-(benzo[d][1,3]dioxol-5-yl)-5-(pyridin-2-yl)-1H-imidazol-2-yl)benzamide301836-41-9
02

Targets

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

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