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A 83-01

Catalog No. T3031   CAS 909910-43-6
Synonyms: ALK5 Inhibitor IV, A8301

A 83-01 (ALK5 Inhibitor IV) is an inhibitor of the TGF-β type I receptors ALK5, ALK4, and ALK7 (IC50=12/45/7.5 nM). A 83-01 promotes the reprogramming of mouse fibroblasts into iPSCs. A 83-01 can be used in organoid cultures.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
A 83-01 Chemical Structure
A 83-01, CAS 909910-43-6
Pack Size Availability Price/USD Quantity
5 mg In stock
$ 52.00
$ 41.60
10 mg In stock
$ 88.00
$ 70.40
25 mg In stock
$ 165.00
$ 132.00
50 mg In stock
$ 269.00
$ 215.20
100 mg In stock
$ 398.00
$ 318.40
500 mg In stock
$ 939.00
$ 751.20
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Purity: 98.76%
Purity: 98%
Purity: 98%
Purity: 97%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description A 83-01 (ALK5 Inhibitor IV) is an inhibitor of the TGF-β type I receptors ALK5, ALK4, and ALK7 (IC50=12/45/7.5 nM). A 83-01 promotes the reprogramming of mouse fibroblasts into iPSCs. A 83-01 can be used in organoid cultures.
Targets&IC50 ALK5:12 nM, ALK4:45 nM, ALK7:7.5 nM
In vitro METHODS: Wild-type mink lung epithelial cells, Mv1Lu, were treated with A 83-01 (0.03-10 μM) and TGF-β (1 ng/mL) for 48 h, and cell proliferation was detected using a Coulter counter.
RESULTS: A 83-01 prevented the inhibition of Mv1Lu cell growth by TGF-β in a dose-dependent manner. [1]
METHODS: Mouse ovarian cancer cells HM-1 were treated with A 83-01 (1-10 μM) for 30 min, followed by treatment with TGF-β (1-10 ng/mL) for 60 min, and the expression levels of target proteins were detected using Western Blot.
RESULTS: The addition of TGF-β1 increased the expression of pSmad3, and A 83-01 inhibited the up-regulation of TGF-β. [2]
In vivo METHODS: To detect anti-tumor activity in vivo, A 83-01 (150 μg/each) was administered intraperitoneally three times a week for four weeks to a B6C3F1 mouse model of peritoneal spread of HM-1 cancer.
RESULTS: Ascites formation tended to be slower in the A 83-01-treated group, and A 83-01 significantly improved the survival rate of the mice. [2]
METHODS: To investigate the role in myocardial injury, A 83-01 (10 mg/kg) was administered intraperitoneally to Nkx2.5 enh-Cre/mTmG mice once daily for seven days.
RESULTS: A 83-01 treatment significantly increased the number of Nkx2.5+ myocardial myofibroblasts at baseline and after myocardial injury, leading to an increase in the number of newly formed myocardial cells. A 83-01 treatment significantly improved ventricular elasticity and stroke work, which led to an improvement of contractility after injury. [3]
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.
Synonyms ALK5 Inhibitor IV, A8301
Molecular Weight 421.52
Formula C25H19N5S
CAS No. 909910-43-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 10 mg/mL (23.72 mM), The compound is unstable in solution. Please use soon.

TargetMolReferences and Literature

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. Cancer Sci. 2005 Nov;96(11):791-800. 2. 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. 3. Chen WP, et al. Pharmacological inhibition of TGFβ receptor improves Nkx2.5 cardiomyoblast-mediated regeneration. Cardiovasc Res. 2015 Jan 1;105(1):44-54. 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.

TargetMolCitations

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

Related compound libraries

This product is contained In the following compound libraries:
TGF-beta/Smad Compound Library Tyrosine Kinase Inhibitor Library Anti-Lung Cancer Compound Library Anti-Ovarian Cancer Compound Library Angiogenesis related Compound Library Reprogramming Compound Library Kinase Inhibitor Library Bioactive Compounds Library Max Inhibitor Library Anti-Obesity Compound Library

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Keywords

A 83-01 909910-43-6 Angiogenesis Stem Cells Tyrosine Kinase/Adaptors ALK TGF-beta/Smad A 8301 ALK5 Inhibitor IV A83-01 Transforming growth factor beta receptors Inhibitor inhibit TGF-β Receptor A8301 A 83 01 inhibitor

 

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