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- RIP kinase
- Nec-4
Nec-4
Nec-4,一个三环衍生物，是受体相互作用蛋白1(RIP1)的一个有效抑制剂，其IC50值为2.6μM，Ki值为0.46μM。
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包装价格促销价数量
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250mg￥0.000.00- +
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500mg￥0.000.00- +
- 货号: ajcx13076
- CAS: 1041644-43-2
- 别名:
- 分子式: C15H13ClFN3O
- 分子量: 305.73
- 纯度: ＞98%
- 溶解度: Soluble in DMSO
- 储存: Store at -20°C
- 库存: 现货
Background
Nec-4, a tricyclic derivative, is a potent receptor interacting protein 1 (RIP1) inhibitor, with an IC50 of 2.6 μM, Ki of 0.46 μM.
Nec-4 (compound 9) is a slightly better competitor than 7 with a lower Ki value that is similar to R-3. Nec-4 is again a slightly better competitor than Rac-3 with Ki and IC50 values comparable to 7 (Nec-4: IC50=2.6±0.1 μM, Ki=0.46±0.05 μM; 7: IC50=10.7±1.8 μM, Ki=4.5±0.9 μM). Overall, all three compounds cross-compete with each other but Nec-4 is able to more effectively displace both 20 and 26 in comparison to the parent compounds Rac-3 and 7, respectively. This suggests that Nec-4 binding likely significantly overlaps with both the Nec-1 and the Nec-3 binding sites.
[1]. Maki JL, et al. Fluorescence polarization assay for inhibitors of the kinase domain of receptor interacting protein 1. Anal Biochem. 2012 Aug 15;427(2):164-74.
