5.04297
受体相互作用蛋白1(RIP1)抑制剂II，7-Cl-O-Nec-1
别名:
受体相互作用蛋白1(RIP1)抑制剂II，7-Cl-O-Nec-1
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关于此项目
经验公式（希尔记法）:
C13H12ClN3O2
化学文摘社编号:
分子量:
277.71
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
SMILES string
Clc1c2[nH]cc(c2ccc1)CC3NC(=O)N(C3=O)C
InChI
1S/C13H12ClN3O2/c1-17-12(18)10(16-13(17)19)5-7-6-15-11-8(7)3-2-4-9(11)14/h2-4,6,10,15H,5H2,1H3,(H,16,19)
InChI key
WIKGAEMMNQTUGL-UHFFFAOYSA-N
assay
≥95% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
off-white to pale yellow
solubility
DMSO: 100 mg/mL
storage temp.
2-8°C
Quality Level
相关类别
Biochem/physiol Actions
主要靶标
RIP1
RIP1
可逆性：是
细胞可渗透性：具有
Disclaimer
毒性：标准处理（A）
General description
一种可渗透细胞的7-氯吲哚基甲基-乙内酰脲，在>400种人类激酶中表现出高度的RIP1选择性抑制活性，并且由于效价（EC50=206 nM，而Nec-1为494 nM，可保护FADD缺陷型Jurkat免受30 h 10 ng/ml TNF-α-诱导的死亡），选择性（对IDO/吲哚胺2，3-脱氧酶无抑制作用，而Nec-1为IC50 = 11.4 µM），代谢稳定性的提高以及体外和体内毒性降低，在阻断RIP1依赖性坏死性凋亡中优于其结构类似物Necrostatin-1（目录号480065）。此外，据报告7-Cl-O-Nec-1在小鼠中表现出血脑屏障渗透性（在雄性小鼠中1 mg/6.25 mL/kg静脉注射后30分钟，脑和血浆浓度分别为0.74和0.31 µM），并且在体内鼠MCAO模型中通过脑室注射（闭塞后18 h控制面积的63%；闭塞后4 h &6 h两次注射8 nmol/2 µL/小鼠）应用时，可有效减少脑梗塞面积。
Other Notes
Ofengeim, D., et al. 2015.Cell Reports10, In press.
Muller, A.J., et al. 2005.Nat. Med.11, 312.
Degterev, A., et al. 2013.Nat. Chem. Biol.9, 192.
Degterev, A., et al. 2013.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.
Teng, X., et al. 2005.Bioorg.Med. Chem. Lett.15, 5039.
Muller, A.J., et al. 2005.Nat. Med.11, 312.
Degterev, A., et al. 2013.Nat. Chem. Biol.9, 192.
Degterev, A., et al. 2013.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.
Teng, X., et al. 2005.Bioorg.Med. Chem. Lett.15, 5039.
Packaging
用惰性气体包装
Preparation Note
仅使用新鲜的DMSO进行溶解。
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。
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Yun Wang et al.
Frontiers in cellular and infection microbiology, 9, 286-286 (2019-08-24)
Programmed cell death and especially necroptosis, a programmed and regulated form of necrosis, have been recently implicated in the progression and outcomes of influenza in mouse models. Moreover, Z-DNA/RNA binding protein 1 (ZBP1) has been identified as a key signaling
Andre L Samson et al.
Nature communications, 11(1), 3151-3151 (2020-06-21)
Mixed lineage kinase domain-like (MLKL) is the terminal protein in the pro-inflammatory necroptotic cell death program. RIPK3-mediated phosphorylation is thought to initiate MLKL oligomerization, membrane translocation and membrane disruption, although the precise choreography of events is incompletely understood. Here, we
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