| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| G408888-1ml |
1ml |
现货  |
|
| 英文别名 | 2H-Indol-2-one, 3-[(3,5-dibromo-4-hydroxyphenyl)methylene]-1,3-dihydro-5-iodo- |
|---|---|
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | GW5074 |
| 生化机理 | GW5074 是一种强效的选择性 c-Raf 抑制剂，IC50 为 9 nM，对 JNK1/2/3、MEK1、MKK6/7、CDK1/2、c-Src、p38 MAP、VEGFR2 或 c-Fms 的活性没有影响。GW5074 可抑制 LK 诱导的细胞凋亡。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | Raf-1 原癌基因抑制剂；丝氨酸/苏氨酸激酶 |
| 产品介绍 |
GW5074 已用作 C2 小鼠骨骼肌成肌细胞、 HT-29 结直肠腺癌细胞系和中性粒细胞中 cRaf1 的特异性抑制剂 Information GW5074 is a potent and selectivec-Rafinhibitor withIC50of 9 nM, no effect on the activities of JNK1/2/3, MEK1, MKK6/7, CDK1/2, c-Src, p38 MAP, VEGFR2 or c-Fms is noted. GW5074 inhibits LK-inducedapoptosis. GW5074 is a potent and specific inhibitor of c-Raf with IC50 of 9 nM and has no effect of MKK6, MKK7, p38 MAP kinase and cdks in vitro. However, treatment of neuronal cultures with GW5074 permits accumulation of activating modifications on c-Raf and also B-Raf. The inhibition of LK-induced apoptosis by GW5074 in cerebellar granule neurons is not MEK-ERK-dependent. GW5074 delays down-regulation of Akt activity but inhibits apoptosis by an Akt-independent mechanism. GW5074 affects Ras, nuclear factor-kappa B and c-jun. GW5074 inhibits cell death caused by neurotoxins in granule cells and other neuronal types. In vivo GW5074 is protective in an in vivo experimental model of Huntington’s disease. GW5074 (5 mg/Kg) completely prevented extensive bilateral striatal lesions induced by 3-NP in mice. GW5074 completely abolishes chronic morphine-mediated AC superactivation I in CHO cells stably expressing the humanμ-opioid receptor. GW5074 suppresses sidestream smoke-induced airway hyperresponsiveness in mice. cell lines： Concentrations：~5 μM Incubation Time：24 hours Powder Purity:≥99% |
| 分子类型 | 小分子 |
|---|---|
| Isomeric SMILES | C1=CC2=C(C=C1I)/C(=C/C3=CC(=C(C(=C3)Br)O)Br)/C(=O)N2 |
| 分子量 | 520.94 |
| Reaxy-Rn | 8641129 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=8641129&ln= |
| 溶解性 | Solubility (25°C) In vitro DMSO: 71 mg/mL (198.64 mM); Water: Insoluble; Ethanol: Insoluble; |
|---|
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