A83-01 is a potent and selective TGF-β pathway inhibitor. It inhibits ALK5 (IC₅₀~12 nM), ALK4 (IC₅₀~45 nM) and ALK7 (IC₅₀~7.5nM). It only has weak inhibitory activity on ALK1, 2, 3, and 6. It blocks phosphorylation of Smad2 and inhibits TGF-β-induced epithelial-to-mesenchymal transition. A83-01 has been used to enhance iPSC reprogramming, induce neural differentiation of human pluripotent stem cells, and promote naïve state of pluripotent stem cells.

How to Use:

In vitro:  A83-01 is typically used at 10 µM as final concentration in cell culture.

In vivo: A83-01 was orally dosed to mice at 100-200 mg/kg once per day or intraperitoneally dosed to mice at 10-100 mg/kg once per day.

Reference:

1. 1.  Tojo M, et al. The ALK-5 inhibitor A-83-01 inhibits smad signaling and epithelial-to-mesenchymal transition by transforming growth factor-beta. (2005) Cancer Science 96 (11), 791-800.
2. 2.  Li W, et al. Generation of rat and human induced pluripotent stem cells by combining genetic reprogramming and chemical inhibitors. (2009) Cell Stem Cell 4(1), 16-19.
3. 3.  Yuan X, et al. Combined Chemical Treatment Enables Oct4-Induced Reprogramming from Mouse Embryonic Fibroblasts. (2011) Stem Cells 29(3), 549–553.
4. 4.  Klincumhom N, et al. Selective TGF-β1/ALK inhibitor improves neuronal differentiation of mouse embryonic stem cells. (2014) Neurosci Lett. 578:1-6. 

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