1. Metabolic Enzyme/Protease Anti-infection Autophagy Apoptosis
  2. Phosphatase HSV Autophagy Apoptosis
  3. Salubrinal

Salubrinal 是有效的选择性 eIF2α 去磷酸化抑制剂。Salubrinal 作为双特异性磷酸酶 2 (Dusp2) 抑制剂,抑制抗胶原蛋白抗体诱导的关节炎。Salubrinal 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 Chemical Structure

CAS No. : 405060-95-9

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥720
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1 mg ¥295
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5 mg ¥650
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10 mg ¥1000
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25 mg ¥2000
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50 mg ¥3500
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100 mg ¥5413
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Top Publications Citing Use of Products

    Salubrinal purchased from MCE. Usage Cited in: Vet Microbiol. 2020 Aug;247:108786.  [Abstract]

    Vero cells are treated with indicated concentrations of Salubrinal for 24 h, then whole cell lysates are collected and subjected to Western blot for eIF2α and P-eIF2α. Salubrinal treatment could block PRV infection-medicated eIF2α dephosphorylation partially.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Salubrinal is a cell-permeable and selective inhibitor of eIF2α dephosphorylation[1]. Salubrinal acts as a dual-specificity phosphatase 2 (Dusp2) inhibitor and suppresses inflammation in anti-collagen antibody-induced arthritis[2]. Salubrinal has antiviral activity against HSV-1 and inhibits dephosphorylation of eIF2α mediated by the HSV-1 protein ICP34.5[3].

    IC50 & Target[1][3]

    Dusp2

     

    HSV-1

     

    体外研究
    (In Vitro)

    Salubrinal, a recently identified PP1 inhibitor capable to protect against endoplasmic reticulum (ER) stress in various model systems, strongly synergized with proteasome inhibitors to augment apoptotic death of different leukemic cell lines. Salubrinal preferentially seems to target the PP1/GADD34 complex, Salubrinal is of interest to examine whether the effect of Salubrinal could also be recapitulated by another inhibitor of this phosphatase. For this purpose cantharidin, wis selected, which is less toxic than okadaic acid, but which also blocks PP1 (IC50=1.7 μM) activities[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    体内研究
    (In Vivo)

    Salubrinal is a synthetic chemical that inhibits de-phosphorylation of eukaryotic translation initiation factor 2 alpha (eIF2α). Salubrinal significantly suppresses inflammation of the paws of CAIA mice. For instance, the clinical scores are 1.94±1.7 (placebo) and 0.31±0.6 (Salubrinal) on day 6; and 4.63±3.4 (placebo) and 1.09±1.6 (Salubrinal) on day 12. Consistent with the clinical scores, the thickening of the paws is also reduced in the Salubrinal-treated group. Furthermore, Salubrinal reduces the histological scores from 1.47±1.10 (N=16; placebo) to 0.59±0.64 (N=16; Salubrinal) (p=0.01)[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    分子量

    479.80

    Formula

    C21H17Cl3N4OS

    CAS 号
    性状

    固体

    颜色

    Light brown to gray

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式

    4°C, protect from light

    *In solvent : -80°C, 2 years; -20°C, 1 year (protect from light)

    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : 50 mg/mL (104.21 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.0842 mL 10.4210 mL 20.8420 mL
    5 mM 0.4168 mL 2.0842 mL 4.1684 mL
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year (protect from light)。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    In Vivo:

    以下溶解方案,请直接配置工作液。建议现用现配,在短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比; 如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶。

    • 方案 一

      请依序添加每种溶剂: 45% PEG300    5% Tween-80    50% Saline

      Solubility: 10 mg/mL (20.84 mM); 悬浊液; 超声助溶

    动物溶解方案计算器
    请输入动物实验的基本信息:

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    由于实验过程有损耗,建议您多配一只动物的量
    计算结果
    工作液所需浓度 : mg/mL
    纯度 & 产品资料

    纯度: 99.69%

    参考文献
    Kinase Assay
    [1]

    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay
    [1]

    Cellular viability is assessed by the WST-1 colorimetric assay. Assays are performed on 96 well plates with 2×104 K562 cells/well in triplicate with Salubrinal concentrations ranging from 5-75 µM (total volume of 200 µL, 18 hrs). Untreated cells served as negative control sample[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [2]

    Mice[2]
    Using Balb/c female mice (~nine weeks old), CAIA is induced by intravenous injection of a 2 mg cocktail of ArthritoMAb antibodies on day 0 followed by intraperitoneal injection of 100 µg LPS on day 3. Mice are randomly divided into a placebo group and a Salubrinal-treated group. Salubrinal (2.0 mg/kg) is intravenously administered daily from day 0, while a solvent (49.5% PEG 400 and 0.5% Tween 80 in PBS) is administered to the placebo group.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    参考文献

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year (protect from light)。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.0842 mL 10.4210 mL 20.8420 mL 52.1050 mL
    5 mM 0.4168 mL 2.0842 mL 4.1684 mL 10.4210 mL
    10 mM 0.2084 mL 1.0421 mL 2.0842 mL 5.2105 mL
    15 mM 0.1389 mL 0.6947 mL 1.3895 mL 3.4737 mL
    20 mM 0.1042 mL 0.5211 mL 1.0421 mL 2.6053 mL
    25 mM 0.0834 mL 0.4168 mL 0.8337 mL 2.0842 mL
    30 mM 0.0695 mL 0.3474 mL 0.6947 mL 1.7368 mL
    40 mM 0.0521 mL 0.2605 mL 0.5211 mL 1.3026 mL
    50 mM 0.0417 mL 0.2084 mL 0.4168 mL 1.0421 mL
    60 mM 0.0347 mL 0.1737 mL 0.3474 mL 0.8684 mL
    80 mM 0.0261 mL 0.1303 mL 0.2605 mL 0.6513 mL
    100 mM 0.0208 mL 0.1042 mL 0.2084 mL 0.5211 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    产品名称:
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    目录号:
    HY-15486
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