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N-Ethylmaleimide (NEM).
N-Ethylmaleimide (NEM) 是一种半胱氨酸蛋白酶抑制剂。N-Ethylmaleimide 特异性抑制线粒体中的磷酸盐转运。
目录号: PC19174 纯度: ≥98%
CAS No. :128-53-0
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中文名称
N-Ethylmaleimide (NEM).
中文别名
N-乙基马来酰亚胺;N-乙基顺丁烯二酰亚胺;(S)-3-氨基四氢吡喃盐酸盐;1-乙基-1H-吡咯-2,5-二酮;N-Ethylmaleimide N-乙基顺丁烯二酰亚胺;N-乙基马来酰亚胺,N-Ethylmaleimide;N-乙基顺丁烯二酰亚胺(NEM);N-乙基顺丁烯二酰亚胺,BR;N-乙基;N-乙基失水苹果酰亚胺;-乙基顺丁烯二酰亚胺;N-乙基顺丁烯二酰;N-乙基顺丁烯二酰亚胺(冷库);N-乙基顺丁烯二酰亚胺 1G;N-乙基马来酰亚胺, 98+%;N-乙基马来酰亚胺, 99+%;N-乙基顺丁烯二酰亚胺(+4℃)
英文名称
N-Ethylmaleimide (NEM)
英文别名
N-Ethylmaleimide;NEM;N-Ethylmaleimide, (NEM);1-Ethyl-1H-pyrrole-2,5-dione~NEM;1-Ethyl-1H-pyrrole-2,5-dione;1-ethylmaleimide;ethvlmaleimide;Ethylmaleimide;n-ethvlmaleimide;N-ethylmaleic imide;n-ethyl-maleimid;N-ethyl-maleimide;N-Ethylmaleinimid;NEMI;NSC 7638;usafb-121;USAF B-121;maleimide, N-ethyl-;1H-pyrrole-2,5-dione, 1-ethyl-;maleic acid N-ethylimide;1-ethylpyrrole-2,5-dione;Maleic Acid-N-Ethylimide;O3C74ACM9V;HDFGOPSGAURCEO-UHFFFAOYSA-N;NEQ;n-ethylmaleimide (nem);N-EM;WLN: T5VNVJ B2;1-ethylazoline-2,5-dione
Cas No.
128-53-0
分子式
C6H7NO2
分子量
125.13
包装储存

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

生物活性

N-Ethylmaleimide (NEM) derives from maleic acid, it can alkylates free sulfhydryl. N-Ethylmaleimide is an irreversible cysteine protease inhibitor. N-ethylmaleimide specific inhibits phosphate transport in mitochondria. N-Ethylmaleimide inhibits prolyl endopeptidase with an IC50 value of 6.3 μM. N-Ethylmaleimide can be used to modify cysteine residues in proteins and peptides.

性状

<43°C Solid,>46°C Liquid

IC50 & Target[1][2]

IC50: 6.3 μM (prolyl endopeptidase)

体外研究(In Vitro)

N-Ethylmaleimide (20 μM;30 min) inhibits Akt Ser-473, Akt Thr-308 , p70S6K, ribosomal protein S6, 4E-BP1, eIF4E, BAD and FKHR-L1 phosphorylation.
N-Ethylmaleimide (20 μM;30 min) affects conversion of pro-caspase-3 in vascular smooth muscle cells.
N-Ethylmaleimide (20 μM;6 h) promotes vascular smooth muscle cells apoptosis.
N-Ethylmaleimide (20 μM;30 min) affects PP2A activity and ROS production in vascular smooth muscle cells.

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

Western Blot Analysis

Cell Line: Vascular smooth muscle cells
Concentration: 20 μM
Incubation Time: 2 hours
Result: Effectively inhibited platelet-derived growth factor-BB (PDGF-BB)-stimulated Akt Ser-473 , Akt Thr-308, p70S6K, ribosomal protein S6, 4E-BP1, BAD and FKHR-L1 phosphorylation with a concentration of 20 μM.

Western Blot Analysis

Cell Line: Vascular smooth muscle cells
Concentration: 20 μM
Incubation Time: 2 hours
Result: Increased of 1.8-fold in the conversion of pro-caspase-3 into active form, and showed better effect with 20 ng/ml PDGF-BB adding.

Apoptosis Analysis

Cell Line: Vascular smooth muscle cells
Concentration: 20 μM
Incubation Time: 6 hours
Result: Induced vascular smooth muscle cells apoptosis by 3-fold, and exhibited 5-fold apoptosis with 20 ng/ml PDGF-BB adding.

Cell Viability Assay

Cell Line: Vascular smooth muscle cells
Concentration: 20 μM
Incubation Time: 30 min
Result: Increased PP2A activity 1.7-flod and increased ROS production 2-fold in vascular smooth muscle cells.
体内研究(In Vivo)

N-Ethylmaleimide (10 mg/kg; i.h.) promotes the prevalence situation of mice with acute gastric ulcers.

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

Animal Model: Male Wistar rats with acute gastric ulcers induced by absolute ethanol injection
Dosage: 10 mg/kg
Administration: Subcutaneous injection; 10 mg/kg once
Result: Increased the lesion area of acute gastric ulcers and attenuated the gastroprotective effect of PAG in rats.
运输条件

Room temperature or refrigerated transportation.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

ClinicalTrial
参考文献
溶解度数据
体外研究: 

DMSO : 50 mg/mL (399.58 mM; Need ultrasonic)

H2O : 50 mg/mL (399.58 mM; Need ultrasonic)

Ethanol : 12.5 mg/mL (99.90 mM; Need ultrasonic)

配制储备溶液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 7.9917 mL 39.9584 mL 79.9169 mL
5 mM 1.5983 mL 7.9917 mL 15.9834 mL
10 mM 0.7992 mL 3.9958 mL 7.9917 mL
*

产品不同,其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液;配成溶液后,建议分装保存,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, 6 months; -20°C, 1 month (protect from light)。-80°C 储存时,建议在 6 个月内使用,-20°C 储存时,建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 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

  • 1.

    建议依照次序添加每种溶剂: PBS

    Solubility: 100 mg/mL (799.17 mM); Clear solution; Need ultrasonic

  • 2.

    建议依照次序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (16.62 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (16.62 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH?O 中,得到澄清透明的生理盐水溶液
  • 3.

    建议依照次序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (16.62 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (16.62 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 4.

    建议依照次序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (16.62 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (16.62 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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