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- IS16601
- 2025年07月23日
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- 详细信息
- 文献和实验
- 技术资料
- 保存条件：
Stroe at -20℃，6 months.
- 保质期：
Stroe at -20℃，6 months.
- 英文名：
Salubrinal(10mM in DMSO,Sterile）
- 库存：
现询
- 供应商：
北京索莱宝科技有限公司
- CAS号：
405060-95-9
- 规格：
1ml
| 基本信息 | |
| CAS | No.405060-95-9 |
| 英文名称 | Salubrinal(10mM in DMSO,Sterile） |
| 分子式 | C21H17Cl3N4OS |
| 分子量 | 479.81 |
| 溶解性 | 请根据自己的实验要求使用。 |
| 外观(性状) | 无菌溶液 |
| 储存条件 | Stroe at -20℃，6 months. |
| 靶点 | eIF2α |
| 通路 | Cell Cycle |
| 背景说明 | Salubrinal是选择性的eIF2α去磷酸化抑制剂。 |
| 生物活性 | Salubrinal is a cell-permeable and selective inhibitor of eIF2α dephosphorylation. Salubrinal acts as a dual-specificity phosphatase 2 (Dusp2) inhibitor and suppresses inflammation in anti-collagen antibody-induced arthritis. Salubrinal has antiviral activity against HSV-1 and inhibits dephosphorylation of eIF2α mediated by the HSV-1 protein ICP34.5.[1-3] |
| 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]. |
| 细胞实验 | 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]. |
| 细胞实验 | 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]. |
| 动物实验 | 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. |
| 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]. |
| 数据来源文献 | [1]. Drexler HC. Synergistic Apoptosis Induction in Leukemic Cells by the Phosphatase Inhibitor Salubrinal and Proteasome Inhibitors. PLoS One. 2009;4(1):e4161. [2]. Hamamura K， et al. Salubrinal acts as a Dusp2 inhibitor and suppresses inflammation in anti-collagen antibody-induced arthritis. Cell Signal. 2015 Apr;27(4):828-35. [3]. Bryant KF， et al. ICP34.5-dependent and -independent activities of salubrinal in herpes simplex virus-1 infected cells. Virology. 2008 Sep 30;379(2):197-204. |
| 单位 | 瓶 |
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文献和实验相关实验
。当然7-AAD会优于PI，因为PI的细胞毒性会更大，而且在流式上的图形也不会像7-AAD漂亮。可以试试。12、受试物的浓度和水溶性问题： 问：向大家请教受试物的问题： (1)我采用是大鼠睾丸支持细胞，染毒的物质是有机磷农药，不溶于水。请问应采用什么样的有机溶剂作为溶剂，要注意什么？ (2)如何确定有机磷农药的染毒浓度？ 答：可以试试DMSO，千分之一体积，不会影响细胞。eg.需要10uM的药液，用DMSO将药配成10mM的储备液，用的时候1000倍稀释。 13、血液中提取单核细胞后的保存问题
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IS16601 Salubrinal(10mM in DMSO,Sterile） 细胞周期 索莱宝
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