N-Ethylmaleimide (Synonyms: N-乙基馬來酰亞胺; NEM)
N-Ethylmaleimide (NEM) 衍生于馬來酸,能烷基化游離巰基,是一種不可逆的 半胱an酸蛋白酶 抑制劑。N-Ethylmaleimide 特異的抑制線粒體中的磷酸鹽轉(zhuǎn)運。N-Ethylmaleimid 對脯氨酰內(nèi)肽酶有抑制作用,其 IC50 值為6.3 μM。N-Ethylmaleimide 可用于修飾蛋白質(zhì)和多肽中的半胱an酸殘基。
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[1][2][3].
IC50 & Target
IC50: 6.3 μM (prolyl endopeptidase)[2]
體外研究(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. |
體內(nèi)研究(In Vivo)
N-Ethylmaleimide (10 mg/kg; i.h.) promotes the prevalence situation of mice with acute gastric ulcers[3].
MCE 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[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. |
Clinical Trial
NCT Number | Sponsor | Condition | Start Date | Phase |
---|---|---|---|---|
NCT00750854 | ESM Technologies, LLC | November 2003 | Not Applicable | |
NCT01407991 | Children′s Hospital of Philadelphia | July 2011 | Phase 2 | |
NCT02751944 | ESM Technologies, LLC | December 2015 | Not Applicable |
分子量:125.13
Formula:C6H7NO2
CAS 號:128-53-0
中文名稱:N-乙基馬來酰亞胺
運輸條件
Room temperature in continental US; may vary elsewhere.
儲存方式
4°C, protect from light
*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶解性數(shù)據(jù)
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)
濃度溶劑體積質(zhì)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 |
請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 儲存時,請在 6 個月內(nèi)使用,-20°C 儲存時,請在 1 個月內(nèi)使用。
以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液,再依次添加助溶劑:
——為保證實驗結(jié)果的可靠性,澄清的儲備液可以根據(jù)儲存條件,適當(dāng)保存;體內(nèi)實驗的工作液,建議您現(xiàn)用現(xiàn)配,當(dāng)天使用; 以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比;如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶
- 1.
請依序添加每種溶劑: PBS
Solubility: 100 mg/mL (799.17 mM); Clear solution; Need ultrasonic
- 2.
請依序添加每種溶劑: 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (16.62 mM); Clear solution
- 3.
請依序添加每種溶劑: 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (16.62 mM); Clear solution
- 4.
請依序添加每種溶劑: 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (16.62 mM); Clear solution
注:產(chǎn)品僅用于科研