Salubrinal

For research use only. Not for use in humans.

目录号:S2923

Salubrinal Chemical Structure

CAS No. 405060-95-9

Salubrinal是一种选择性eIF2α去磷酸化抑制剂,可以抑制ER应激介导的细胞凋亡,无细胞试验中EC50约为15 μM。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 2297.41 现货
RMB 1214.29 现货
RMB 3660.93 现货
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客户使用Selleck生产的Salubrinal发表文献23篇:

产品安全说明书

PERK抑制剂选择性比较

生物活性

产品描述 Salubrinal是一种选择性eIF2α去磷酸化抑制剂,可以抑制ER应激介导的细胞凋亡,无细胞试验中EC50约为15 μM。
靶点
eIF2α [1]
(Cell-free assay)
体外研究

Salubrinal是一种选择性细胞复合体抑制剂,使真核翻译起始因子2亚基α(eIF2α)去磷酸化。Salubrinal抑制蛋白糖基化抑制剂Tunicamycin(TM)诱导的ER应激介导的细胞凋亡,这种作用具有剂量依赖性,半数有效浓度(EC50)为15 μM。Salubrinal在caspase-7加工过程中,也抑制TM诱导的DNA断裂,ER应激激活caspase-7。然而,Salubrinal不是一般的凋亡抑制剂。Salubrinal作用于PC12细胞,快速且强效诱导eIF2α磷酸化及其下游效应,包括下调cyclin D1和上调GADD34和CHOP,eIF2α磷酸化诱导GADD34和CHOP这两种蛋白质的表达。Salubrinal通过抑制PP1/GADD34复合体,而抑制eIF2α去磷酸化。Salubrinal通过抑制eIF2α去磷酸化,而抑制HSV复制,IC50为3μM。[1]Salubrinal增强非快速眼动(NREM)睡眠。[2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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HAL-01 NVfTdohxT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NWPUTGl{UW6qaXLpeIlwdiCxZjDoeY1idiCKQVytNFEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NEA:KDlwM{G1NFUh|ryPLh?= Mn:4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVgxOTJ5Lze+V2FPT0WUPD;hQi=>
EB-3 NY\BWFE3T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NF\oR3VKdmirYnn0bY9vKG:oIHj1cYFvKEWELUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3MDC9JFkvPjJ3N{Kg{txONg>? NYrHeYhmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOThyMUK3M{c,W0GQR1XSQE9iRg>?
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Ramos-2G6-4C10 NWTxPGNrT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NF73WYZKdmirYnn0bY9vKG:oIHj1cYFvKFKjbX;zMVJIPi12Q{GwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUCgQUA6NjlyM{G1JO69VS5? NFHUeGk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQDBzMkevK|5USU6JRWK8M4E,
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RCC10RGB NV;QTHdwT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MknTTY5pcWKrdHnvckBw\iCqdX3hckBTS0NzMGLHRkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwJF0hOjJwNkG0OkDPxE1w MoPhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVgxOTJ5Lze+V2FPT0WUPD;hQi=>
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... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
ATF4 ; 

PubMed: 27729194     


OVCAR10 cells were incubated with sub-lethal dose of Salubrinal [20 μM] for 1, 3, 6, 12, 24 and 48 h. Whole cell lysates were subjected to Western blot analysis and probed with the above antibodies.

HSF1 / p-HSF1 / ATF3 / c-fos / NFATc1 / RelA ; 

PubMed: 27189267     


The accumulation of cellular transcription factors in nucleus was analyzed after treatment with salubrinal for 4 hours.

GRP78 / p-eIF2α / CHOP ; 

PubMed: 24525736     


HepG2 cells were treated with salubrinal at the indicated dosages for 24 h. Total proteins were harvested and subjected to western blotting analysis of GRP78, P-eIF2α, CHOP and β-actin. 

27729194 27189267 24525736
体内研究 Salubrinal处理小鼠角膜感染的模型,抑制HSV复制。与对照组比,Salubrinal局部处理,显著降低感染动物眼拭子中恢复的病毒滴度。[1]Salubrinal脑室内给药处理,显著改变稳态睡眠响应。[3]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

细胞实验:[1]
- 合并
  • Cell lines: PC12
  • Concentrations: 0-100 μM
  • Incubation Time: 48 小时
  • Method: PC12细胞按每孔5000个接种在383孔板中,孔中为含3μg/ml TM 的40μL无酚红培养基,诱导ER应激。通过自动化针转移将100 nL DiverSet E (5 mg/mlin DMSO) 或美国国家癌症研究所(NCI) 结构多样性设置和开放性收集 (10 mM,溶于DMSO) (NCI)加入到孔中。48小时后,通过发光ATP实验测定细胞活力。每组实验板上DMSO和zVAD.fmk处理的孔分别作为阴性和阳性对照,缓解ER应激诱导的ATP损耗。
    (Only for Reference)
动物实验:[1]
- 合并
  • Animal Models: 8周大的雄性CD-1远交系小鼠
  • Dosages: 75μM
  • Administration: 角膜上滴定
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 95 mg/mL (197.99 mM)
Water Insoluble
Ethanol '2 mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 479.81
化学式

C21H17Cl3N4OS

CAS号 405060-95-9
储存条件 粉状
溶于溶剂
别名 N/A

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID