A 83-01 is a selective inhibitor of TGF-β type I receptor ALK5 kinase, type I activin/nodal receptor ALK4 and type I nodal receptor ALK7 with IC50 values of 12 nM, 45 nM and 7.5 nM, respectively.

A-83-01 (4?μM) treatment increases myotube formation, the expression of MyHC and the expression of Myf5 and MyoD in C2C12 cells[1]. Expression of pSmad3 is increased by the addition of TGF-β1, and the effects of TGF-β1 are inhibited in ovarian cancer cells by A-83-01. TGF-β1 increases cell motility, adhesion and invasion, while A-83-01 decreases these behaviors in HM-1 cells[2]. A-83-01 treatment significantly increases these parameters within 24 h that is positively related to pericyte coverage and tumor cell proliferation. Apparent diffusion coefficient (ADC) determined by diffusion-weighed imaging is decreased by A-83-01 treatment, suggesting the decrease of tumor interstitial fluid pressure[3].

A-83-01 (50, 150 and 500 μg/mouse, i.p.) significantly improves survival of the mice without body weight or neurobehavioral appearances[2]. A-83-01 (0.5 mg/kg, i.p.) shows a significantly stronger antitumor effect in mice bearing M109 cells[4].

HM-1 cells are seeded into a 96-well plate and are incubated for 18 hr. A-83-01 (1 μM) or vehicle are then added for 12 hr followed by the addition of TGF-β1 (1 ng/mL) or vehicle for 60 hr. The number of viable cells in each well is examined using the WST-1 assay following the manufacturer's instructions.

909910-43-6

C25H19N5S

421.52

ALK5 Inhibitor IV;A 83-01

[1]Wei-jian L I, Zhen-yu W, Tian-jie Y, et al. The study of immortalized hepatocyte-derived liver progenitor-like cells used in bioartificial liver therapy[J]. Chinese Hepatolgy. 24(8): 871. [2]Kawano K, Maitani Y. Tumor permeability of nanocarriers observed by dynamic contrast-enhanced magnetic resonance imaging. Yakugaku Zasshi. 2010 Dec;130(12):1679-85. [3]Gong-Bo Fu, Wei-Jian Huang, Min Zeng, Xu Zhou, Hong-Ping Wu, Chang-Cheng Liu, Han Wu, Jun Weng, Hong-Dan Zhang, Yong-Chao Cai, Charles Ashton, Min Ding, Dan Tang, Bao-Hua Zhang, Yi Gao, Wei-Feng Yu, Bo Zhai, Zhi-Ying He, Hong-Yang Wang, and He-Xin Yan . Expansion and differentiation of human hepatocyte-derived liver progenitor-like cells and their use for the study of hepatotropic pathogens [J]. Cell Research. 2019 Jan;29(1):8-22. [4]Taniguchi, Y., Kawano, K., Minowa, T., Sugino, T., Shimojo, Y., & Maitani, Y. (2010). Enhanced antitumor efficacy of folate-linked liposomal doxorubicin with TGF-β type I receptor inhibitor. Cancer Science, 101(10), 2207-2213. doi: 10.1111/j.1349-7006.2010.01646.x [5]Yamamura S, et al. The activated transforming growth factor-beta signaling pathway in peritoneal metastases is a potential therapeutic target in ovarian cancer. Int J Cancer. 2012 Jan 1;130(1):20-8.

[1]Fu G B, Huang W J, Zeng M, et al. Expansion and differentiation of human hepatocyte-derived liver progenitor-like cells and their use for the study of hepatotropic pathogens. Cell Research. 2019, 29(1): 8-22 [2]Ma X, Lu Y, Zhou Z, Human expandable pancreatic progenitor–derived β cells ameliorate diabetes. Science Advances. 2022, 8(8): eabk1826. [3]He W, Zhu X, Xin A, et al. Long-term maintenance of human endometrial epithelial stem cells and their therapeutic effects on intrauterine adhesion. Cell & Bioscience. 2022, 12(1): 1-20. [4]Zhang S W, Chen W, Lu X, et al. An efficient and user‐friendly method for cytohistological analysis of organoids. Journal of Tissue Engineering and Regenerative Medicine. 2021

DMSO:>10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years