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产品名称
Necrostatin-1, Necrostatin-1, CAS 4311-88-0, is a cell-permeable, potent, and selective blocker of necroptosis (EC₅₀ = 494 nM in FADD-deficient Jurkat cells treated with TNF-α).
质量水平
方案
≥95% (HPLC)
表单
crystalline solid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
颜色
yellow
溶解性
DMSO: 10 mg/mL
methanol: 5 mg/mL
运输
ambient
储存温度
2-8°C
SMILES字符串
S=C1NC(C(=O)N1C)Cc2c3c([nH]c2)cccc3
InChI
1S/C13H13N3OS/c1-16-12(17)11(15-13(16)18)6-8-7-14-10-5-3-2-4-9(8)10/h2-5,7,11,14H,6H2,1H3,(H,15,18)
InChI key
TXUWMXQFNYDOEZ-UHFFFAOYSA-N
一般描述
坏死性凋亡的细胞可渗透，强效和选择性阻滞剂（在用TNF-α处理的FADD缺陷型Jurkat细胞中EC50=494 nM），是一种由死亡域受体（DRs）介导的非凋亡性坏死性细胞死亡途径，可在缺血性脑损伤小鼠模型中提供神经保护。对DR诱导的凋亡没有影响。还充当RIP1激酶的选择性和ATP竞争性抑制剂，对RIP2激酶活性的影响可忽略不计。Nec-1靶标似乎是执行事件上游和DR下游的关键常见坏死性凋亡步骤。也可以使用非活性对照Nec-1i（目录号480066）。
坏死性凋亡的细胞可渗透，强效和选择性阻滞剂（在用TNF-α处理的FADD缺陷型Jurkat细胞中EC50=494 nM），是一种由死亡域受体（DRs）介导的非凋亡性坏死性细胞死亡途径，可在缺血性脑损伤小鼠模型中提供神经保护。对DR诱导的凋亡没有影响。还充当RIP1激酶的选择性和ATP竞争性抑制剂，对RIP2激酶活性的影响可忽略不计。Nec-1靶标似乎是执行事件上游和DR下游的关键常见坏死性凋亡步骤。也可以使用非活性对照Nec-1i（目录号480066）。也可以25 mM的DMSO溶液（货号505224）提供。
生化/生理作用
主要靶标
坏死性凋亡的阻滞剂
坏死性凋亡的阻滞剂
产物与ATP竞争。
可逆：否
在阻断用TNF-处理的FADD缺陷型Jurkat细胞的坏死中EC50=494 nMα
细胞可渗透性：具有
包装
用惰性气体包装
警告
毒性：标准处理（A）
重悬
复溶后，等分并冷冻保存（-20°C）。贮备液在-20°C下可稳定保存至多3个月。
其他说明
Degterev, A., et al. 2013.Nat. Chem. Biol.9, 192.
Degterev, A., et al. 2012.Cell Death Differ.20, 366.
Christofferson, D.E., et al. 2012.Cell Death Dis.3, e320.
Takahashi, N., et al. 2012.Cell Death Dis.3, e437.
Degterev, A., et al. 2008.Nat. Chem. Biol.4, 313.
Degterev, A., et al. 2005.Nat. Chem. Biol.1, 112.
Muller, A.J., et al. 2005.Nat. Med.11, 312.
Teng, X., et al. 2005.Bioorg.Med. Chem. Lett.15, 5039.
Degterev, A., et al. 2012.Cell Death Differ.20, 366.
Christofferson, D.E., et al. 2012.Cell Death Dis.3, e320.
Takahashi, N., et al. 2012.Cell Death Dis.3, e437.
Degterev, A., et al. 2008.Nat. Chem. Biol.4, 313.
Degterev, A., et al. 2005.Nat. Chem. Biol.1, 112.
Muller, A.J., et al. 2005.Nat. Med.11, 312.
Teng, X., et al. 2005.Bioorg.Med. Chem. Lett.15, 5039.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
Roberto Fernández-Acosta et al.
Molecules (Basel, Switzerland), 27(13) (2022-07-10)
The use of nanomaterials rationally engineered to treat cancer is a burgeoning field that has reported great medical achievements. Iron-based polymeric nano-formulations with precisely tuned physicochemical properties are an expanding and versatile therapeutic strategy for tumor treatment. Recently, a peculiar
Peng He et al.
Cell death discovery, 10(1), 255-255 (2024-05-25)
Caspase-8 (Casp8) serves as an initiator of apoptosis or a suppressor of necroptosis in context-dependent manner. Members of the p90 RSK family can phosphorylate caspase-8 at threonine-265 (T265), which can inactivate caspase-8 for bypassing caspase-8-mediated blockade of necroptosis and can
Chi G Weindel et al.
Cell, 185(17), 3214-3231 (2022-07-31)
Although mutations in mitochondrial-associated genes are linked to inflammation and susceptibility to infection, their mechanistic contributions to immune outcomes remain ill-defined. We discovered that the disease-associated gain-of-function allele Lrrk2G2019S (leucine-rich repeat kinase 2) perturbs mitochondrial homeostasis and reprograms cell death
Sasker Grootjans et al.
Nature protocols, 11(8), 1444-1454 (2016-07-16)
Several cell death assays have been developed based on a single biochemical parameter such as caspase activation or plasma membrane permeabilization. Our fluorescent apoptosis/necrosis (FAN) assay directly measures cell death and distinguishes between caspase-dependent apoptosis and caspase-independent necrosis of cells
Bolin Hou et al.
Cell death discovery, 8(1), 319-319 (2022-07-14)
The underlying mechanism by which growth factor receptor-bound protein 2 (Grb2) regulates necroptosis remains unexplored. In the present study, we found that rasfonin, a fungal natural product and an activator of necroptosis, enhanced Grb2 binding to receptor-interacting serine/threonine kinase 1
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