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- 2025年07月08日
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- 详细信息
- 文献和实验
- 技术资料
- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 6 months; -20°C, 1 month.
- 英文名：
HTS466284
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
396129-53-6
- 规格：
10 mM * 1 mL/5 mg/10 mg/50 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥605.0 |
|---|---|---|---|
| 规格： | 5 mg | 产品价格： | ￥550.0 |
| 规格： | 10 mg | 产品价格： | ￥760.0 |
| 规格： | 50 mg | 产品价格： | ￥2750.0 |
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LY-364947
CAS No. : 396129-53-6
MCE 国际站：LY-364947
产品活性：LY-364947 (HTS466284) 是一种有效的，ATP 竞争性的 TGFβR-I 抑制剂，IC50 值为 59 nM，是对 TGFβR-II 选择性的 7 倍。
研究领域：TGF-beta/Smad
作用靶点：TGF-β Receptor
In Vitro: LY-364947 is an ATP competitive and tight-binding inhibitor, inhibiting phosphorylation of P-Smad3 by TGFβR-I Kinase with Ki of 28 nM. LY-364947 inhibits in vivo Smad2 phosphorylation within the NMuMg cells with IC50 of 135 nM. LY-364947 reverses TGF-β-mediated growth inhibition in NMuMg cells with IC50 of 0.218 μM. LY-364947 potentiates the xVent2-lux BMP4 response in NMuMg cells by 30% at concentrations as low as 0.25 μM. LY-364947 (2 μM) prevents TGF-β-induced epithelial?mesenchymal transition in NMuMg cells. LY-364947 (3 μM) induces expression of Prox1 and LYVE-1 in almost all HDLECs after 24 hours. LY-364947 promotes nuclear export of Foxo3a, with low Smad2/3 and high Akt phosphorylation levels in leukaemia-initiating cells. LY-364947 (< 20 μM) suppresses leukaemia-initiating cells colony-forming ability after co-culture with OP-9 stromal cells.
In Vivo: LY-364947 (1 mg/kg, i.p.) accelerates lymphangiogenesis, as evidence by significantly increasing the LYVE-1-positive areas in a mouse model of chronic peritonitis. LY-364947 (1 mg/kg, i.p.) significantly increases the LYVE-1-positive areas in tumor tissues in tumor xenograft models using BxPC3 pancreatic adenocarcinoma cells. LY-364947 (25 mg/kg) increases p-Akt and decreases nuclear Foxo3a in leukaemia-initiating cells in CML-affected mice.
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文献和实验刘淼清 在园中看到关于LY294002和Wortmannin区别。（建议用LY，主要原因有两个，一，Wortmannin相对来说要贵好多；二，更重要的，Wortmannin半衰期很短，如果没记错的话大概只有8－10小时，所以如果处理时间久的话，药物浓度下降很快。有篇文献研究了Wortmannin的半衰期，有兴趣可以去查查看，应该是2005年的文献。 ） 这篇文献不知有哪位战友知道。 第二 LY294002的半衰期是多少
olivial 最近在做细胞内信号转导通路PI-3K-Akt，关于它的抑制剂LY 294002的配制，说明书上写用DMSO，在做实验时设了vehicle（含等量DMSO）组，但发现DMSO对细胞（小胶质细胞）有影响，且DMSO与干预药有协同作用，MTT结果显示DMSO浓度>=0.1%即对细胞造成损伤，而任何浓度DMSO（0.01%~0.1%）都与干预药有协同作用，乙醇的结果亦如此。所以想请教，大家在配LY时是怎么配的？在使用LY时是否遇到了上述问题
Determining Ligand Specificity of Ly49 Receptors
Ly49 receptors in rodents, like KIR in humans, play an integral role in the regulation of NK cell activity. Some inhibitory Ly49 are known to interact with specific MHC I alleles to maintain tolerance to self tissues, and NK activation
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