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Necrostatin-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.
Necrostatin-1 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.
|Storage||Store at RT|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
The following data is based on the product molecular weight 259.33. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|0.3 mM||12.85 mL||64.27 mL||128.54 mL|
|1.5 mM||2.57 mL||12.85 mL||25.71 mL|
|3 mM||1.29 mL||6.43 mL||12.85 mL|
|15 mM||0.26 mL||1.29 mL||2.57 mL|
References are publications that support the biological activity of the product.
Degterev et al (2005) Chemical inhibitor of nonapoptotic cell death with therapeutic potential for ischemic brain injury. Nat.Chem.Biol. 1 112 PMID: 16408008
Degterev et al (2008) Identification of RIP1 kinase as a specific cellular target of necroSTAT. Nat.Chem.Biol. 4 313 PMID: 18408713
Linkermann et al (2012) Rip1 (receptor-interacting protein kinase 1) mediates necroptosis and contributes to renal ischemia/reperfusion injury. 81 751 PMID: 22237751
If you know of a relevant reference for Necrostatin-1, please let us know.
Keywords: Necrostatin-1, Necrostatin-1 supplier, non-apoptotic, cell, death, necroptosis, Death, domain, receptor-associated, adaptor, RIP1, inhibits, inhibitors, Apoptosis, RIPK, RIPK1, receptor-interacting, protein, kinase, 1, other, kinases, Necroptosis, RIP, Kinases, 2324, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for Necrostatin-1 include:
Kim (2017) Shikonin-induced necroptosis is enhanced by the inhibition of autophagy in non-small cell lung cancer cells Journal of Translational Medicine 15 123 PMID: 28569199
Chefetz et al (2019) A Pan-ALDH1A Inhibitor Induces Necroptosis in Ovarian Cancer Stem-like Cells. Cell Rep 26 3061 PMID: 30865894
Greer et al (2018) ONC201 kills breast cancer cells in vitro by targeting mitochondria. Oncotarget 9 18454 PMID: 29719618
Sagher et al (2014) The small molecule NSC676914A is cytotoxic and differentially affects NFκB signaling in ovarian cancer cells and HEK293 cells. Cancer Cell Int 14 75 PMID: 25324692
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Combinatorial treatments of Necrostatin-1 with other chemotherapeutic drugs were performed to elucidate the dependance of the latter on the induction of necroptosis. Results were consistent.
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.