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Signaling Pathway

A 83-01

HY-10432

(A83-01; A-83-01)

A 83-01

A 83-01 Chemical Structure

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 (IC50 values are 12, 45 and 7.5 nM respectively).

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50 mg $405 In-stock
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10 mg €137 In-stock
50 mg €397 In-stock
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Product name: A 83-01
Cat. No.: HY-10432

A 83-01 Data Sheet

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    Purity: 97.61%

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    DataSheet

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Biological Activity of A 83-01

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 (IC50 values are 12, 45 and 7.5 nM respectively).
IC50 Value: 12 nM ( ALK5)
Target: ALK5
A 83-01 blocks phosphorylation of Smad2 and inhibits TGF-β-induced epithelial-to-mesenchymal transition. A 83-01 only weakly inhibits ALK-1, -2, -3, -6 and MAPK activity and is more potent than SB 431542.
in vitro:  A-83-01, an inhibitor of TGF-β type I receptor, increased the expression of Myf5 and MyoD, and enhanced myotube formation [1].  Microarray analysis of HM-1 cells treated with TGF-β1 and/or A-83-01 revealed that A-83-01 efficiently inhibited transcriptional changes that are induced by TGF-β1 [2]. -83-01 treatment significantly increased these parameters within 24 h that was positively related to pericyte coverage and tumor cell proliferation. Furthermore, apparent diffusion coefficient (ADC) determined by diffusion-weighed imaging was decreased by A-83-01 treatment, suggesting the decrease of tumor interstitial fluid pressure. Vascular function of the tumor improved by A-83-01treatment well assessed on post-Gd-L-enhanced MR images [3].
in vivo: The targeting efficacy of single intravenous injections of F-SL combined with A-83-01 was evaluated by measurement of the biodistribution and the antitumor effect in mice bearing murine lung carcinoma M109. A-83-01 temporarily changed the tumor vasculature around 3 h post injection. A-83-01 induced 1.7-fold higher drug accumulation of F-SL in the tumor than liposome alone at 24 h post injection [4].

Protocol (Extracted from published papers and Only for reference)

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Chemical Information

M.Wt 421.52 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C25H19N5S
CAS No 909910-43-6
Solvent & Solubility

50 mM in DMSO

Preparing Stock Solutions

1 mg 5 mg 10 mg
1 mM 2.3724 mL 11.8618 mL 23.7237 mL
5 mM 0.4745 mL 2.3724 mL 4.7447 mL
10 mM 0.2372 mL 1.1862 mL 2.3724 mL

References on A 83-01

Inhibitor Kit

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