A TGF-β type I receptor inhibitor
A 83-01 is an inhibitor of TGF-β type I receptor kinase (ALK5), activin type IB receptor (ALK4), and nodal type I receptor (ALK7) (IC50s = 12, 45, and 7.5 nM, respectively).1 It blocks the phosphorylation of SMAD2/3 and inhibits TGF-β-induced epithelial-to-mesenchymal transition.1 It has little effect on bone morphogenic type I receptors, p38 mitogen-activated protein kinase, or ERK.1 A 83-01 has been used to reprogram fibroblasts into alternative lineages, including neural stem cells and cardiomyocytes.2,3
1.Tojo, M., Hamashima, Y., Hanyu, A., et al.The ALK-5 inhibitor A-83-01 inhibits Smad signaling and epithelial-to-mesenchymal transition by transforming growth factor-βCancer Sci.96(11)791-800(2005) 2.Cao, N., Huang, Y., Zheng, J., et al.Conversion of human fibroblasts into functional cardiomyocytes by small moleculesScience352(6290)1216-1220(2016) 3.Zhang, M., Lin, Y.H., Sun, Y.J., et al.Pharmacological reprogramming of fibroblasts into neural stem cells by signaling-directed transcriptional activationCell Stem Cell18(5)653-667(2016)
动态评分
0.0