A-83-01 is an ALK inhibibitor. It was found that A-83-01 inhibited the transcriptional activity induced by TGF-beta type I receptor ALK-5 and that by activin type IB receptor ALK-4 and nodal type I receptor ALK-7, the kinase domains of which are structurally highly related to those of ALK-5. A-83-01 was found to be more potent in the inhibition of ALK5 than a previously described ALK-5 inhibitor, SB-431542, and also to prevent phosphorylation of Smad2/3 and the growth inhibition induced by TGF-beta. A-83-01 inhibited the epithelial-to-mesenchymal transition induced by TGF-beta, suggesting that A-83-01 and related molecules may be useful for preventing the progression of advanced cancers.
CAS Number: 909910-43-6
Molecular Weight: 421.52
Chemical Name: 3-(6-methylpyridin-2-yl)-N-phenyl-4-(quinolin-4-yl)-1H-pyrazole-1-carbothioamide
Appearance: white solid powder
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Soluble in DMSO, not in water
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥720 days if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
A83-01 is typically used at 10 µM as final concentration in cell culture.
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.
- 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.
- i 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.
- Yuan X, et al. Combined Chemical Treatment Enables Oct4-Induced Reprogramming from Mouse Embryonic Fibroblasts. (2011) Stem Cells 29(3), 549¨C553.
- Klincumhom N, et al. Selective TGF-β1/ALK inhibitor improves neuronal differentiation of mouse embryonic stem cells. (2014) Neurosci Lett. 578:1-6.
Products are for research use only. Not for human use.
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