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Submit ReviewNecrostatin-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 Kinase Inhibitor Library. 了解 Tocris 化合物库的更多信息。
分子量 | 259.33 |
公式 | C13H13N3OS |
储存 | Store at RT |
纯度 | ≥98% (HPLC) |
CAS Number | 4311-88-0 |
PubChem ID | 2828334 |
InChI Key | TXUWMXQFNYDOEZ-UHFFFAOYSA-N |
Smiles | CN1C(=S)NC(CC2=CNC3=CC=CC=C23)C1=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 7.78 | 30 |
以下数据基于产品分子量 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.
浓度/溶剂体积/质量 | 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 |
参考文献是支持产品生物活性的出版物。
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.
关键词: 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
引用文献是使用了 Tocris 产品的出版物。 Necrostatin-1 的部分引用包括:
Greer et al (2018) ONC201 kills breast cancer cells in vitro by targeting mitochondria. Oncotarget 9 18454 PMID: 29719618
Chefetz et al (2019) A Pan-ALDH1A Inhibitor Induces Necroptosis in Ovarian Cancer Stem-like Cells. Cell Rep 26 3061 PMID: 30865894
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
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.