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| 品牌 | absin | CAS | 396129-53-6 |
|---|---|---|---|
| 分子式 | C17H12N4 | 纯度 | ＞98% |
| 分子量 | 272.3 | 货号 | abs810425 |
| 规格 | 5mg | 供货周期 | 现货 |
| 主要用途 | is a potent ATP-competitive inhibitor o | 应用领域 | 化工,生物产业,农林牧渔,制药/生物制药,综合 |
LY-364947 396129-53-6
| 产品描述 | |
| 描述 | LY-364947 is a potent ATP-competitive inhibitor of TGFβR-I with IC50 of 59 nM, shows 7-fold selectivity over TGFβR-II. |
| 纯度 | >98% |
| 储存/保存方法 | Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 别名 | LY 364947；LY364947；HTS466284 |
| 外观 | White to beige Powder |
| 可溶性/溶解性 | DMSO ：20 mg/mL (73.45 mM) |
| 生物活性 | |
| 靶点 | TGFβRI；RIPK2；CK1δ；TGFβRII；MLK-7K |
| In vitro(体外研究) | LY364947 is an ATP competitive and tight-binding inhibitor, inhibiting phosphorylation of P-Smad3 by TGFβR-I kinase with Ki of 28 nM. LY364947 inhibits in vivo Smad2 phosphorylation within the NMuMg cells with IC50 of 135 nM. LY364947 reverses TGF-β-mediated growth inhibition in NMuMg cells with IC50 of 0.218 μM. LY364947 potentiates the xVent2-lux BMP4 response in NMuMg cells by 30% at concentrations as low as 0.25 μM. LY364947 (2 μM) prevents TGF-β-induced epithelial−mesenchymal transition in NMuMg cells. LY364947 (3 μM) induces expression of Prox1 and LYVE-1 in almost all HDLECs after 24 hours. LY364947 promotes nuclear export of Foxo3a, with low Smad2/3 and high Akt phosphorylation levels in leukaemia-initiating cells. LY364947 ( |
| In vivo(体内研究) | LY364947 (1 mg/kg i.p.) accelerates lymphangiogenesis, as evidence by significantly increased the LYVE-1-positive areas, in a mouse model of chronic peritonitis. LY364947 (1 mg/kg i.p.) significantly increases the LYVE-1-positive areas in tumor tissues in tumor xenograft models using BxPC3 pancreatic adenocarcinoma cells. LY364947 (25 mg /kg) increases p-Akt and decreases nuclear Foxo3a in leukaemia-initiating cells in CML-affected mice. |
| 研究领域 | |
| 研究领域 | Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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