LDN-212854 is primarily used in research settings for its potent and selective antagonism of the TGF-β type I receptor, also known as ALK5. This activity makes it a valuable tool in studies related to fibrosis, where it helps inhibit the signaling pathway responsible for excessive extracellular matrix deposition. It has shown utility in cellular models of tissue scarring, including in the liver, lungs, and kidneys, aiding the development of potential anti-fibrotic therapies. Additionally, LDN-212854 is employed in cancer research due to the involvement of TGF-β signaling in tumor progression and immune evasion. By blocking ALK5, it can help restore immune surveillance and reduce epithelial-to-mesenchymal transition (EMT), a process linked to tumor metastasis. Its use in in vitro and in vivo models supports the investigation of novel oncology treatments, particularly those combining immunotherapy with pathway inhibition. The compound is also applied in stem cell and developmental biology studies, where modulation of TGF-β signaling influences cell differentiation and maintenance of pluripotency. Due to its selectivity and efficacy, LDN-212854 enables precise control over this pathway, making it a preferred choice in mechanistic studies and preclinical validation of therapeutic targets.