ALK5 Inhibitor II (hydrochloride)

- Overview
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    Background
    
    IC50: 4, 18, and 23 nM for ALK5 autophosphorylation, TGF-β cellular assay, and ALK5 binding in HepG2 cells, respectivelyALK5 Inhibitor II is an ALK5 inhibitor.The TGF-beta family of cytokines signal via serine/threonine kinase transmembrane type I and type II receptors. Binding TGF-beta1 to the receptor complex triggers activation of activin receptor-like kinase (ALK), initiating downstream signaling involving Smad transcription factors, mitogen-activated protein kinases, and PI3K-Akt signaling. ALK5 can phosphorylate Smad2 and Smad3, while ALK1 activates Smad1 and Smad5, triggering their translocation to the nucleus together with Smad4.In vitro: ALK5 inhibitor II was identified as a cell permeable, selective inhibitor of the TGF-β type 1 activin like kinase receptor ALK5. ALK5 inhibitor II showed less potent activity (IC50s > 16 μM) when tested against a panel of 9 related kinases, including p38 MAPK and GSK3. In addition, when cocrystallized with ALK5, ALK5 inhibitor II was found to be able to bind in the ATP site with the 1,5-naphthyridine N5 interacting with the backbone NH of His-283 [1].In vivo: Up to now, there is no animal in vivo reported.Clinical trial: So far, no clinical study has been conducted.
- Properties
  - Alternative Name
    
    E 616452,RepSox,SJN 2511; 2-(3-(6-methylpyridin-2-yl)-1H-pyrazol-4-yl)-1,5-naphthyridine, monohydrochloride
    
    Molecular Formula
    
    C17H13N5·HCl
    
    Molecular Weight
    
    323.8
    
    Appearance
    
    A crystalline solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≤0.5mg/ml in ethanol
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

ALK5 Inhibitor II (hydrochloride)

ALK5 Inhibitor II (hydrochloride)

Background

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