| 包装 | 价格(元) |
| 1mg | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 别名 | E 616452,RepSox,SJN 2511 |
| 化学名 | 2-(3-(6-methylpyridin-2-yl)-1H-pyrazol-4-yl)-1,5-naphthyridine, monohydrochloride |
| Canonical SMILES | CC1=NC(C2=NNC=C2C3=NC4=CC=CN=C4C=C3)=CC=C1.Cl |
| 分子式 | C17H13N5o HCl |
| 分子量 | 323.8 |
| 溶解度 | ≤0.5mg/ml in ethanol |
| 储存条件 | Store at -20℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | 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: |
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