ALK5 Inhibitor II (hydrochloride)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
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).
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 323.8 |
Formula | C17H13N5·HCl |
Synonyms | E 616452,RepSox,SJN 2511 |
Solubility | ≤0.5mg/ml in ethanol |
Chemical Name | 2-(3-(6-methylpyridin-2-yl)-1H-pyrazol-4-yl)-1,5-naphthyridine, monohydrochloride |
SDF | Download SDF |
Canonical SMILES | CC1=NC(C2=NNC=C2C3=NC4=CC=CN=C4C=C3)=CC=C1.Cl |
运输条件 | 蓝冰运输或根据您的需求运输。 |
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