in MD2-IN-1
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- 更新时间 2019/7/11 16:25:40
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MedChemExpress (MCE) 专注于为科学家提供高品质的生物活性小分子化合物，化合物库及各类试剂盒，总部位于美国新泽西。
• MedChemExpress (MCE) 产品作用于 20 多个热门信号通路及研究领域的300多个细分靶点，拥有 10000 特异性抑制剂、激动剂，以及 50 活性化合物筛选库；
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抑制剂，调节剂，API，天然产物，各种类型化合物库
| 供货周期 | 现货 | 规格 | 10 mM * 1 mL；1 mg；5 mg |
|---|---|---|---|
| 货号 | HY-103483 | 应用领域 | 生物产业 |
MD2-IN-1
产品活性：MD2-IN-1 是髓样分化蛋白 2 (MD2) 的抑制剂，对重组人 MD2 (rhMD2) 的 KD 值为 189 μM。
研究领域：Immunology/Inflammation
作用靶点：Toll-like Receptor (TLR)
In Vitro: Myeloid differentiation protein 2 (MD2) is a co-receptor of TLR4. Among those derivatives, MD2-IN-1 (compound 20) shows the strongest inhibitory effect on LPS-induced expression of both TNF-α and IL-6. Compare to the vehicle, LPS alone largely increases the amount of TLR4/MD2 complex, while pretreatment with MD2-IN-1 inhibits the increase of TLR4/MD2 complex to the vehicle level. SPR analysis shows that MD2-IN-1 exhibits recognizable binding to rhMD2 protein in a dose-dependent manner, with a KD value of 189 μM, while the KD value of xanthohumol binding to MD2 is 460 μM. Pre-treatment with different doses of MD2-IN-1 dose-dependently reduces FITC-LPS binding to MD2 in cell surface membranes, with a 65% inhibition at 10 μM in terms of mean fluorescence intensity. Pretreatment with MD2-IN-1 also dose-dependently blocks LPS-induced MAPK phosphorylation in the MPMs.
In Vivo: Administration of MD2-IN-1 evidently reduces the LPS-induced increase in protein concentrations in BALF. The lung wet/dry weight ratio is markedly higher in the LPS-treated group than the control group, and MD2-IN-1 treatment reduces LPS-induced pulmonary edema. LPS also causes observable lung histopathologic changes, including areas of inflammatory infiltration, hemorrhage, interstitial edema, thickening of the alveolar wall, and lung tissue destruction. These histopathological changes are ameliorated in the MD2-IN-1 treatment group.
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