SB-431542

• GMP format available

SB-431542 is a potent and selective inhibitor of the transforming growth factor-β (TGF-β) type I receptor, specifically targeting ALK4, ALK5, and ALK7. It is a cell-permeable compound that effectively inhibits SMAD2 phosphorylation, with IC₅₀ values of 140 nM and 94 nM for ALK4 and ALK5, respectively.

This compound is widely used in research to study TGF-β signaling pathways and has applications in various biological processes, including the suppression of TGF-β-induced proliferation in human osteosarcoma cells and the reprogramming of fibroblasts into induced pluripotent stem cells (iPSCs), as well as apoptosis and growth suppression. Additionally, SB-431542 has been shown to improve the efficiency of generating human iPSCs and is used in protocols for differentiating stem cells into specific cell types.

Key features and applications include:

• Cancer Research: SB-431542 is used to investigate the role of TGF-β signaling in cancer progression and metastasis. It helps in understanding how TGF-β influences tumor growth and the tumor microenvironment.
• Stem Cell Research: It is employed to study the differentiation of stem cells. By inhibiting TGF-β signaling, researchers can explore how stem cells differentiate into various cell types.
• Tissue Engineering: SB-431542 is used in tissue engineering to control the differentiation of cells and to prevent fibrosis in engineered tissues.

Relevant disease states include:

• Fibrosis: SB-431542 is used to study and potentially treat various fibrotic diseases. For example, it has been shown to prevent arthrofibrosis, a condition characterized by joint stiffening and scar tissue formation.
• Muscle Injuries: It has been used in research to reduce fibrosis and fatty infiltration in muscle injuries, such as rotator cuff tears.