Chemical Name: 5-(1H-Indol-3-ylmethyl)-3-methyl-2-thioxo-4-imidazolidinone
Biological ActivityNecrostatin-1 is an ATP-competitive, allosteric inhibitor of receptor-interacting protein kinase 1 (RIPK1) (EC50 = 182 nM). Blocks non-apoptotic cell death via inhibition of a specific cellular pathway, necroptosis, which leads to necrosis (EC50 = 494 nM). Reduces ischemic brain injury in a mouse model of stroke.
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Chemical inhibitor of nonapoptotic cell death with therapeutic potential for ischemic brain injury.
Degterev et al.
Identification of RIP1 kinase as a specific cellular target of necroSTAT.
Degterev et al.
Citations for Necrostatin-1
The citations listed below are publications that use Tocris products. Selected citations for Necrostatin-1 include:
4 Citations: Showing 1 - 4
A Pan-ALDH1A Inhibitor Induces Necroptosis in Ovarian Cancer Stem-like Cells.
Authors: Chefetz Et al.
Cell Rep 2019;26:3061
ONC201 kills breast cancer cells in vitro by targeting mitochondria.
Authors: Greer Et al.
Shikonin-induced necroptosis is enhanced by the inhibition of autophagy in non-small cell lung cancer cells
Journal of Translational Medicine 2017;15(1):123
The small molecule NSC676914A is cytotoxic and differentially affects NFκB signaling in ovarian cancer cells and HEK293 cells.
Authors: Sagher Et al.
Cancer Cell Int 2014;14:75
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100nM of Nec-1 was used to inhibit RIPK1 after administration cells with TNFa, zVADfmk, and smac inhibitors to induce necroptosis, then cell death rate was measured with a commercial kit.