Salubrinal

For research use only. Not for use in humans.

目录号：S2923

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
5mg	RMB 1214.29	现货
25mg	RMB 3660.93	现货
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客户使用Selleck生产的Salubrinal发表文献23篇：

Nat Commun, 2021, 12(1):1589

PubMed: 33707434 ( click the link to review the publication )

Int J Mol Sci, 2021, 22(7)3501

PubMed: 33800699 ( click the link to review the publication )

Adv Sci (Weinh), 2020, 7(22):2002747

PubMed: 33240783 ( click the link to review the publication )

Cell Death Dis, 2020, 11(9):766

PubMed: 32943607 ( click the link to review the publication )

Mol Hum Reprod, 2020, 26(1):30-39

PubMed: 31814016 ( click the link to review the publication )

Infect Immun, 2020, 20 pii: IAI

PubMed: 32312764 ( click the link to review the publication )

J Biosci, 2020, 45:71

PubMed: 32457283 ( click the link to review the publication )

Toxicol Lett, 2020, 322:77-86

PubMed: 31931077 ( click the link to review the publication )

J Biol Chem, 2019, 294(19):7755-7768

PubMed: 30914477 ( click the link to review the publication )

Mol Hum Reprod, 2019, 10.1093/molehr/gaz002

PubMed: 30657961 ( click the link to review the publication )

DNA Cell Biol, 2019, 10.1089/dna.2019.5097

PubMed: 31809190 ( click the link to review the publication )

Mol Nutr Food Res, 2018, 62(8):e1700890

PubMed: 29446867 ( click the link to review the publication )

Neuropharmacology, 2018, 130:77-91

PubMed: 29197516 ( click the link to review the publication )

Neural Regen Res, 2018, 13(5):827-836

PubMed: 29863013 ( click the link to review the publication )

Reproduction, 2018, 155(6):493-503

PubMed: 29764928 ( click the link to review the publication )

Anat Rec (Hoboken), 2018, 301(8):1390-1397

PubMed: 29698579 ( click the link to review the publication )

Oncogenesis, 2017, 6(5):e341

PubMed: 28530706 ( click the link to review the publication )

Neurotox Res, 2017, 31(2):204-217

PubMed: 27848175 ( click the link to review the publication )

Oncotarget, 2016, 7(29):45715-45729

PubMed: 27304189 ( click the link to review the publication )

Sci Rep, 2016, 6:34330

PubMed: 27680712 ( click the link to review the publication )

Viruses, 2016, 8(2)

PubMed: 26907328 ( click the link to review the publication )

Oncotarget, 2016, 7(17):23860-73

PubMed: 27009865 ( click the link to review the publication )

J Am Soc Nephrol, 2014, 10.1681/ASN.2013121332

PubMed: 25398788 ( click the link to review the publication )

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	Activity Description	PMID
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no-11	MlKwS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	MkjSTY5pcWKrdHnvckBw\iCqdX3hckBvdy1zMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyIE2gOFgvQTl{MzFOwG0v	MmPjQIEhfGG{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 Mol Oncol 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 Sci Rep The accumulation of cellular transcription factors in nucleus was analyzed after treatment with salubrinal for 4 hours. GRP78 / p-eIF2α / CHOP ; PubMed: 24525736 Cell Death Dis 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]

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)

参考文献

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 Download Salubrinal SDF

分子量	479.81
化学式	C₂₁H₁₇Cl₃N₄OS
CAS号	405060-95-9
储存条件	3年-20°C 粉状 2年-80°C 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

每只动物给药体积

动物数量

只

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

计算结果:

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

注意：1. 首先保证母液是澄清的；
2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

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

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
初始浓度:
稀释倍数:

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

通过输入化合物的化学式来计算其分子量：

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

如果有其他问题，请给我们留言。

研究领域

产品类型

定制您的化合物库

Salubrinal

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

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)

参考文献

溶解度 (25°C)

化学数据 Download Salubrinal SDF

动物体内配方计算器 (澄清溶液)

计算器

摩尔浓度计算器

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

摩尔浓度计算公式

稀释计算器

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

连续稀释计算器方程

连续稀释

计算结果

分子量计算器

总分子量：g/mol

摩尔浓度计算器

技术支持