CAS號	128-53-0	產(chǎn)地	國產(chǎn)
規(guī)格	10mg	級別	化工級
證書	ISO系列證書

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(yùn)。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	Osteoarthritis\|Fibromyalgia	November 2003	Not Applicable
NCT01407991	Children′s Hospital of Philadelphia	Enteral Tube Placement	July 2011	Phase 2
NCT02751944	ESM Technologies, LLC	Exercise-induced Joint Pain Stiffness and Cartilage Turnover	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(yùn)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)

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)

配制儲備液

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。

In Vivo:

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