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A 83-01 sodium salt

Catalog No. T10442   CAS 2828431-89-4

A 83-01 sodium salt is a potent inhibitor of TGF-β type I receptor ALK5 kinase, ALK4 and ALK7, with IC 50 s of 12 nM, 45 nM and 7.5 nM against the ALK5, ALK4 and ALK7 induced transcription, respectively [1].

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A 83-01 sodium salt Chemical Structure
A 83-01 sodium salt, CAS 2828431-89-4
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Biological Description
Chemical Properties
Storage & Solubility Information
Description A 83-01 sodium salt is a potent inhibitor of TGF-β type I receptor ALK5 kinase, ALK4 and ALK7, with IC 50 s of 12 nM, 45 nM and 7.5 nM against the ALK5, ALK4 and ALK7 induced transcription, respectively [1].
Targets&IC50 ALK7 cell-based:7.5 nM , ALK5, cell-based:12 nM , ALK4 cell-based:45 nM
In vitro A 83-01 sodium salt is a potent inhibitor of TGF-β type I receptor ALK5 kinase, type I activin/nodal receptor ALK4 and type I nodal receptor ALK7, reduces the level of ALK-5-induced transcription with an IC 50 of 12 nM in Mv1Lu cells, also blocks the ALK4-TD and ALK7-TD induced transcription with IC 50 s of 45 nM and 7.5 nM in R4-2 cells, and weakly suppresses that induced by constitutively active ALK-6, ALK-2, ALK-3, and ALK-1. A 83-01 (0.03-10 μM) potently prevents the growth-inhibitory effects of TGF-β, and completely inhibits the effect at 3 μM. A 83-01 (1-10 μM) inhibits TGF-β-induced Smad activation in HaCaT cells [1]. A 83-01 (1 μM) decreases cell motility, adhesion and invasion increased by TGF-β1 in HM-1 cells while not change cell proliferation [2].
In vivo A 83-01 (50, 150 and 500 μg/mouse, i.p.) markedly improves survival of the mice without body weight or neurobehavioral appearances [2]. A 83-01 (0.5 mg/kg, i.p.) shows a significantly strong antitumor effect in mice bearing M109 cells [3].
Molecular Weight 444.51
Formula C25H19N5NaS+
CAS No. 2828431-89-4

Storage

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

Solubility Information

DMSO: 100 mg/mL (224.97 mM), sonification is recommended.

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. Taniguchi Y, et al. Enhanced antitumor efficacy of folate-linked liposomal doxorubicin with TGF-β type I receptor inhibitor. Cancer Sci. 2010 Oct;101(10):2207-13.

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Keywords

A 83-01 sodium salt 2828431-89-4 Angiogenesis Tyrosine Kinase/Adaptors ALK A 83 01 sodium salt A 8301 sodium salt A 83-01 sodium inhibitor inhibit

 

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