N-Ethylmaleimide (NEM) 衍生于马来酸，能烷基化游离巯基，是一种不可逆的半胱氨酸蛋白酶抑制剂。N-Ethylmaleimide 特异的抑制线粒体中的磷酸盐转运。N-Ethylmaleimid 对脯氨酰内肽酶有抑制作用，其IC50值为6.3 μM。N-Ethylmaleimide 可用于修饰蛋白质和多肽中的半胱氨酸残基。
| 生物活性 | N-Ethylmaleimide (NEM) derives from maleic acid, it can alkylates free sulfhydryl. N-Ethylmaleimide is an irreversiblecysteine proteaseinhibitor. N-ethylmaleimide specific inhibits phosphate transport in mitochondria. N-Ethylmaleimide inhibitsprolyl endopeptidasewith anIC50value of 6.3 μM. N-Ethylmaleimide can be used to modify cysteine residues in proteins andpeptides[1][2][3]. |
| IC50& Target | IC50: 6.3 μM (prolyl endopeptidase)[2] |
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[2].N-Ethylmaleimide (20 μM;30 min) affects conversion of pro-caspase-3 in vascular smooth muscle cells[2].N-Ethylmaleimide (20 μM;6 h) promotes vascular smooth muscle cells apoptosis[2].N-Ethylmaleimide (20 μM;30 min) affects PP2A activity and ROS production in vascular smooth muscle cells[2].
Western Blot Analysis[2] | 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[2] | 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[2] | 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[2] | 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. |
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体内研究
(In Vivo) | N-Ethylmaleimide (10 mg/kg; i.h.) promotes the prevalence situation of mice with acute gastric ulcers[3].
| Animal Model: | Male Wistar rats with acute gastric ulcers induced by absolute ethanol injection[3] | | 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. |
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| 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, 6 months; -20°C, 1 month (protect from light) |
| 溶解性数据 | In Vitro: 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) 配制储备液 | 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 |
*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℃, 6 months; -20℃, 1 month (protect from light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro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. 请依序添加每种溶剂： PBS Solubility: 100 mg/mL (799.17 mM); Clear solution; Need ultrasonic 2. 请依序添加每种溶剂： 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。 3. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin 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 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 4. 请依序添加每种溶剂： 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。 *以上所有助溶剂都可在本网站选购。
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