A83-01 is a selective inhibitor of the transforming growth factor-beta type I receptor ALK5, the Nodal receptor ALK4, and the nodal receptor ALK7
Targets
Target
Value
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.[1]
In Vitro
A 83-01, an ALK4/5/7 inhibitor, was used in rat cardiac fibroblasts to block Activin A-induced Smad2/3 phosphorylation, reducing collagen production by about 50% and cell proliferation by 40% in vitro. This suggests A 83-01 can effectively suppress fibrosis-related changes in these cells.[1]
References
Yamamura, S., Matsumura, N., Mandai, M., Huang, Z., Oura, T., Baba, T., Hamanishi, J., Yamaguchi, K., Kang, H. S., Okamoto, T., Abiko, K., Mori, S., Murphy, S. K., & Konishi, I. (2012). The activated transforming growth factor-beta signaling pathway in peritoneal metastases is a potential therapeutic target in ovarian cancer. International Journal of Cancer, 130(1), 20–28. [PMID: 20811699]
Chen, W.-P., Wu, S.-M., & Huang, Y.-C. (2015). Activin A protects against cardiac fibrosis through the Smad2/3 signaling pathway. Cardiovascular Research, 105(1), 44–54. [PMID: 25344366]
Store lyophilized at -20ºC, keep desiccated. In lyophilized form, the chemical is stable for 36 months. In solution, store at -20ºC and use within 1 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.
Solubility
In vitro
DMSO
21 mg/mL (49.82 mM)
Water
<1 mg/mL
Ethanol
<1 mg/mL
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
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