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Biological Description

Description: 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.

Targets&IC50: ALK5:12 nM, ALK4:45 nM, ALK7:7.5 nM

In vitro: A-83-01 (4?μM) treatment increases myotube formation, the expression of MyHC and the expression of Myf5 and MyoD in C2C12 cells. 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.

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

Cell Research: 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.

Chemical Properties

Molecular Weight: 421.52

Formula: C25H19N5S

CAS No.: 909910-43-6

Storage & Solubility Information

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: >10 mM

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Catalog #: T3031

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References and Literature

1. 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.

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. 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

4. 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.

5. 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.