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GSK963 是手性的选择性受体相互作用蛋白 1 酶抑制剂,其IC50值为 29 nM。它在体外强效选择性抑制小鼠和人细胞的坏死。

GSK963 是手性的选择性受体相互作用蛋白 1 酶抑制剂,其IC50值为 29 nM。它在体外强效选择性抑制小鼠和人细胞的坏死。
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 1 mg | ¥ 315 | In stock | |
| 2 mg | ¥ 453 | In stock | |
| 5 mg | ¥ 747 | In stock | |
| 10 mg | ¥ 1,230 | In stock | |
| 25 mg | ¥ 2,490 | In stock | |
| 50 mg | ¥ 3,930 | In stock | |
| 100 mg | ¥ 5,630 | In stock | |
| 1 mL x 10 mM (in DMSO) | ¥ 822 | In stock |
GSK963 相关产品
| 产品描述 | GSK963 (Racemate), a structurally distinct, potent and selective inhibitor of RIP1 kinase(IC50=29 nM). |
| 靶点活性 | RIP1:29 nM |
| 体外活性 | GSK 963在体外相对于Nec-1显示出更高的效能,此增强效力亦在TNF+zVAD诱导的无菌性休克模型中体现为更高的疗效。以2 mg/kg的剂量,GSK 963能够完全抑制TNF+zVAD引起的温度下降,这一表型与最近描述的RIP1激酶失活敲入小鼠的表型相符。在这个急性模型中,GSK 963不同剂量对温度下降的抑制水平与基于GSK 963药代动力学特性和体外效力模型预测的疗效相一致。 |
| 体内活性 | GSK 963在啮齿类和人类细胞中高效阻断坏死性细胞死亡,其IC50值分别为1 nM和4 nM。相比之下,不活跃的类似物GSK 962在这些测试中的效力至少低1000倍。 |
| 激酶实验 | GSK′963 was tested against 339 kinases using a P33-radiolabeled assay at Reaction Corp Biology. The compound was tested at a single dose in duplicate at 10?μM. Reactions were carried out at 10?μM ATP. Data are reported as % enzyme activity (relative to DMSO controls). |
| 别名 | GSK963 (Racemate) |
| 分子量 | 230.31 |
| 分子式 | C14H18N2O |
| CAS No. | 2049868-46-2 |
| Smiles | CC(C)(C)C(=O)N1N=CC[C@H]1c1ccccc1 |
| 密度 | 1.06 g/cm3 (Predicted) |
| 颜色 | White |
| 物理性状 | Solid |
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| 溶解度信息 | DMSO: 40 mg/mL (173.68 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
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