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- ALK5 Inhibitor II (hydrochloride)
ALK5 Inhibitor II (hydrochloride)
A selective inhibitor of ALK5
此产品仅用于科学研究，我们不为任何个人用途提供产品和服务
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包装价格促销价数量
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1mg￥562.00450.00- +
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5mg￥1100.00880.00- +
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10mg￥1900.001520.00- +
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25mg￥4000.003200.00- +
- 货号: ajcx11062
- CAS: N/A
- 别名: E 616452,RepSox,SJN 2511
- 分子式: C17H13N5 ? HCl
- 分子量: 323.8
- 纯度: ＞98%
- 溶解度: ≤0.5mg/ml in ethanol
- 储存: Store at -20°C
- 库存: 现货
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).
