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ALK5 Inhibitor II (hydrochloride)

Catalog No.
C3656
ALK5 inhibitor
Grouped product items
SizePriceStock Qty
5mg
$71.00
Ship with 5-10 days
10mg
$126.00
Ship with 5-10 days
25mg
$270.00
Ship with 5-10 days

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

IC50: 4, 18, and 23 nM for ALK5 autophosphorylation, TGF-β cellular assay, and ALK5 binding in HepG2 cells, respectively

ALK5 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.

Reference:
[1] Gellibert, F. ,Wollven, J.,Fouchet, M.H., et al. Identification of 1,5-naphthyridine derivatives as a novel series of potent and selective TGF-β type I receptor inhibitors. Journal of Medicinal Chemistry 47(18), 4494-4506 (2004).

Chemical Properties

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt323.8
FormulaC17H13N5·HCl
SynonymsE 616452,RepSox,SJN 2511
Solubility≤0.5mg/ml in ethanol
Chemical Name2-(3-(6-methylpyridin-2-yl)-1H-pyrazol-4-yl)-1,5-naphthyridine, monohydrochloride
SDFDownload SDF
Canonical SMILESCC1=NC(C2=NNC=C2C3=NC4=CC=CN=C4C=C3)=CC=C1.Cl
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Quality Control

Quality Control & MSDS

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Chemical structure

ALK5 Inhibitor II (hydrochloride)