Necrostatin-1

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Chemical Structure| 4311-88-0 同义名 : Nec-1
CAS号 : 4311-88-0
货号 : A181851
分子式 : C13H13N3OS
纯度 : 99%+
分子量 : 259.33
MDL号 : MFCD00056916
存储条件：

Pure form Inert atmosphere, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 45 mg/mL(173.53 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
靶点

  • TNF-α

    RIP1, EC50:490 nM
描述 Necrostatin-1 (Nec-1) serves as a potent inhibitor of necroptosis, capable of crossing the blood-brain barrier, with an effective concentration (EC50) of 490 nM in Jurkat cells. It specifically inhibits RIP1 kinase activity (EC50=182 nM) and also functions as an inhibitor of IDO[1].
作用机制 Necrostatin 1 is a small molecular that specifically and potently inhibits cell death caused by the stimulation of death-domain receptors in the presence of caspase inhibition. The inhibition of Necrostatin 1 on RIP1 activity was through the T-loop segment.
细胞研究
细胞系 浓度 检测类型 检测时间 活性说明 数据源
8505c 100 μM Cell Viability Assay 24 h increases cellular survival 22136818
A549 50 μM Cell Viability Assay 24 h inhibits MMS-induced cell death 26472723
AGS 60 μm Cell Viability Assay 1 h prevents shikonin-induced cell death 24463199
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.86mL

0.77mL

0.39mL

19.28mL

3.86mL

1.93mL

38.56mL

7.71mL

3.86mL
参考文献

[1]Degterev A, et al. Chemical inhibitor of nonapoptotic cell death with therapeutic potential for ischemic brain injury. Nat Chem Biol. 2005 Jul;1(2):112-9.

[2]Linkermann A, et al. The RIP1-kinase inhibitor necrostatin-1 prevents osmotic nephrosis and contrast-induced AKI in mice. J Am Soc Nephrol. 2013 Oct;24(10):1545-57.

[3]Feyen D, et al. Increasing short-term cardiomyocyte progenitor cell (CMPC) survival by necrostatin-1 did not further preserve cardiac function. Cardiovasc Res. 2013 Jul 1;99(1):83-91.