A 83-01

A 83-01 is a potent and selective small-molecule inhibitor targeting the TGF-β type I receptor kinase (ALK5), activin type IB receptor (ALK4), and nodal type I receptor (ALK7) with an IC₅₀ of 12 nM, 45 nM, and 7.5 nM, respectively. It inhibits phosphorylation of Smad2/3, thereby blocking TGF-β-induced epithelial-to-mesenchymal transition (EMT), a key process in fibrosis and cancer metastasis. A 83-01 is widely used in research to modulate TGF-β signaling pathways, particularly in studies involving fibrosis, cancer, and stem cell biology.

Key features and applications include:

• Selective Inhibition: Targets ALK5/4/7 with high potency, effectively blocking Smad2/3 phosphorylation.Cancer Research: Suppresses epithelial-to-mesenchymal transition (EMT), a key process in tumor metastasis.
• Fibrosis Models: Reduces fibroblast activation and extracellular matrix deposition in models of liver, lung, and skin fibrosis.
• Stem Cell Studies: Enhances reprogramming efficiency and supports maintenance of pluripotency in iPSCs and ESCs.
• Cardiovascular Regeneration: Promotes cardiomyocyte proliferation and repair in heart injury models.
• Wound Healing: Modulates TGF-β signaling to improve tissue regeneration and reduce scarring.

Relevant disease states include:

• Cancer: A 83-01 is used to study mechanisms of metastasis and drug resistance in cancers such as breast, pancreatic, and colorectal cancer.
• Fibrotic Diseases: It is a valuable tool in preclinical models of pulmonary, hepatic, and dermal fibrosis, where TGF-β plays a central role in pathological tissue remodeling.
• Cardiovascular Disease: By modulating TGF-β signaling, A 83-01 supports research into myocardial repair and prevention of cardiac fibrosis.
• Regenerative Medicine: Its role in maintaining stem cell pluripotency and promoting tissue regeneration makes it relevant in wound healing and organ repair studies.