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Salubrinal

Salubrinal

产品编号 T3045   CAS 405060-95-9

Salubrinal 是一种磷酸酶抑制剂 ,对真核翻译起始因子 2 亚基 (eIF2α) 发挥作用。它作为双特异性磷酸酶 2 抑制剂,抑制抗胶原蛋白抗体诱导的关节炎。它具有抗HSV-1病毒的活性,并抑制由HSV-1蛋白 ICP34.5 介导的eIF2α的去磷酸化。

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Salubrinal Chemical Structure
Salubrinal, CAS 405060-95-9
规格 价格/CNY 货期 数量
1 mg ¥ 239 现货
2 mg ¥ 333 现货
5 mg ¥ 538 现货
10 mg ¥ 828 现货
25 mg ¥ 1,660 现货
50 mg ¥ 2,890 现货
100 mg ¥ 4,330 现货
500 mg ¥ 9,360 现货
1 mL * 10 mM (in DMSO) ¥ 597 现货
产品目录号及名称: Salubrinal (T3045)
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选择批次  
纯度: 100%
纯度: 99.97%
纯度: 98.25%
纯度: 98.16%
更多批次查询请联系客服
生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Salubrinal, a phosphatases (PP1) inhibitor(IC50=1.7 μM), exhibits function on the eukaryotic translation initiation factor 2 subunit (eIF2α).
靶点活性 PP1:1.7 μM
体外活性 在小鼠角膜感染的模型中,Salubrinal抑制HSV复制,降低感染动物眼拭子中病毒滴度.在脑室内给药Salubrinal,能够显著改变稳态睡眠响应.
体内活性 Salubrinal(EC50=15 μM)以剂量依赖的方式抑制衣霉素诱导的ER应激,诱导细胞凋亡。Salubrinal(IC50=3 μM)通过抑制eIF2α去磷酸化,而抑制HSV复制。在C12细胞中,Salubrinal下调cyclin D1和上调GADD34和CHOP。
激酶实验 Phosphatase activities are determined on immunoprecipitates of the phosphatases. Briefly, 2×106 K562 cells are treated for 18 hr with Salubrinal (20 μM), PSI (10 nM), the combination of both drugs or okadaic acid (100 nM). After washing with PBS, cells are lysed for 15 min on ice either in PP1LB (for determination of PP1γ-activity; 20 mM Tris-HCl, pH 7.5, 1% Triton X-100, 10% glycerol, 132 mM NaCl, Roche complete protease inhibitor ) or in RIPA (for PP2A), supplemented with Roche complete protease inhibitor). Cell lysates containing 500 μg (PP1γ) or 300 μg (PP2A) protein are immunoprecipitated overnight at 4°C with 2-3 μg of the appropriate antibodies and then incubated with Protein A-Sepharose. Immunoprecipitates are washed three times in lysis buffer, followed by resuspension in phosphatase assay buffer (PP2A: 20 mM Tris-HCl, pH7.5, 0.1 mM CaCl2; PP1γ: 50 mM Tris HCl pH 7.0, 0.2 mM MnCl2, 0.1 mM CaCl2, 125 μg/mL BSA, 0.05% Tween 20), supplemented with 100 μM 6,8-difluoro-4-methyl-umbelliferyl phosphate (DiFMUP). Precipitates are allowed to react with substrate for 1 hr at 37°C on an Eppendorf Thermoshaker, centrifuged and DiFMU fluorescence is measured on a BioTek Lambda Fluoro 320 microplate reader (360 nmex/460 nmem). Phosphatase activities are given as percent change relative to the control (DMSO treated cells)[1].
细胞实验 PC12 cells are plated in 384-well plates at 5000 cells per well in 40μL phenol red-freemedium containing 3μg/ml Tm to induce ER stress. 100 nL of the DiverSet E (5 mg/mlin DMSO) or National Cancer Institute's (NCI) Structural Diversity set and Open Collections (10 mM in DMSO) (NCI) are added to the wells by robotic pin transfer. After 48 hours, cell viability is assessed using a luminescence-based ATP assay. DMSO- and zVAD.fmk-treated wells on each plate served as negative and positive controls for rescue from ER stress-induced ATP loss, respectively.(Only for Reference)
分子量 479.81
分子式 C21H17Cl3N4OS
CAS No. 405060-95-9

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 48 mg/mL (100 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0842 mL 10.4208 mL 20.8416 mL 52.104 mL
5 mM 0.4168 mL 2.0842 mL 4.1683 mL 10.4208 mL
10 mM 0.2084 mL 1.0421 mL 2.0842 mL 5.2104 mL
20 mM 0.1042 mL 0.521 mL 1.0421 mL 2.6052 mL
50 mM 0.0417 mL 0.2084 mL 0.4168 mL 1.0421 mL
100 mM 0.0208 mL 0.1042 mL 0.2084 mL 0.521 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Boyce M, et al. Science, 2005, 307(5711), 935-939. 2. Methippara MM, et al. Am J Physiol Regul Integr Comp Physiol, 2009, 296(1), 178-184. 3. Methippara M, Neuroscience, 2012, 209, 108-118. 4. Zhang J, Zhang P, Meng C, et al. The PERK Pathway Plays a Neuroprotective Role During the Early Phase of Secondary Brain Injury Induced by Experimental Intracerebral Hemorrhage[M]//. Subarachnoid Hemorrhage. Springer, Cham, 2020: 105-119. 5. Meng C, Zhang J, Dang B, et al. PERK pathway activation promotes intracerebral hemorrhage induced secondary brain injury by inducing neuronal apoptosis both in vivo and in vitro[J]. Frontiers in neuroscience. 2018 Feb 28;12:111.

文献引用

1. Meng C, Zhang J, Dang B, et al. PERK pathway activation promotes intracerebral hemorrhage induced secondary brain injury by inducing neuronal apoptosis both in vivo and in vitro. Frontiers in Neuroscience. 2018 Feb 28;12:111 2. Zhao Y, Feng Y, Ye Q, et al.The oral microbiome in young women at different stages of periodontitis: Prevotella dominant in stage III periodontitis.Frontiers in Cellular and Infection Microbiology.2022 3. Berthier A, Gheeraert C, Johanns M, et al.The Molecular Circadian Clock Is a Target of Anti-cancer Translation Inhibitors.Journal of Biological Rhythms.2023: 07487304231202561.
Vidarabine FIT-039 Surfactin Guanosine Tiglic acid Kushenol W Aquacycline LDC4297

相关化合物库

该产品包含在如下化合物库中:
抗衰老化合物库 已知活性化合物库 抑制剂库 HIF-1化合物库 人代谢物化合物库 抗感染化合物库 自噬库 细胞凋亡化合物库 抗代谢疾病化合物库 共价抑制剂库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
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% Tween 80
% ddH2O
计算 重置

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Salubrinal 405060-95-9 Apoptosis Autophagy Metabolism Microbiology/Virology Phosphatase PERK HSV Herpes simplex virus Inhibitor inhibit inhibitor

 

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