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N-Ethylmaleimide/N-乙基马来酰亚胺 {[allProObj[0].p_purity_real_show]}

货号:A175883 同义名: N-乙基顺丁烯二酰亚胺 / NEM; NSC 7638

N-Ethylmaleimide是一种不可逆的半胱氨酸肽酶抑制剂,是一种来源于马来酸的有机化合物。

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There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
N-Ethylmaleimide/N-乙基马来酰亚胺 化学结构 CAS号:128-53-0
N-Ethylmaleimide/N-乙基马来酰亚胺 化学结构
CAS号:128-53-0
N-Ethylmaleimide/N-乙基马来酰亚胺 3D分子结构
CAS号:128-53-0
N-Ethylmaleimide/N-乙基马来酰亚胺 化学结构 CAS号:128-53-0
N-Ethylmaleimide/N-乙基马来酰亚胺 3D分子结构 CAS号:128-53-0
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N-Ethylmaleimide/N-乙基马来酰亚胺 纯度/质量文件 产品仅供科研

货号:A175883 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Cysteine Protease 其他靶点 纯度
Z-FA-FMK 99%+
Leupeptin hemisulfate 97%
PMSF 95%
PD 151746 +

m-calpain, IC50: 5.33 μM

μ-Calpain, IC50: 260 nM

95%
Odanacatib ++++

Cathepsin K (human), IC50: 0.2 nM

Cathepsin K (rabbit), IC50: 1 nM

99%+
E-64 +++

Cysteine protease, IC50: 9 nM

99%+
E 64c 95%
E-64d 99%+
MG-101 98%+
Calpeptin ++

Calpain II (porcine kidney), ID50: 40 nM

Calpain I (porcine erythrocytes), ID50: 52 nM

98%+
Cathepsin inhibitor 1 +++

Cathepsin L, pIC50: 7.9

Cathepsin L2, pIC50: 5.5

98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

N-Ethylmaleimide/N-乙基马来酰亚胺 生物活性

描述 N-Ethylmaleimide (NEM), a reagent that alkylates free sulfhydryl groups, is a cysteine protease inhibitor[2]. N-ethylmaleimide (NEM) was shown to be a highly effective inhibitor of the following coupled mitochondrial processes: oxidative phosphorylation, ATP-32Pi exchange, Pi-induced light scattering and configurational changes, State III respiration, valinomycin-induced translocation of potassium with Pi as the anion, and calcium accumulation in presence of Pi. Also NEM, even et levels 2-3 times greater than those required to inhibit oxidative phosphorylation in intact mitochondria, did not inhibit coupled processes in submitochondrial particles[3]. When D. salina thylakoid membranes are treated with N-ethylmaleimide, both photophosphorylation and the inducible CF1 ATPase activity are partially (approx. 60%) inhibited. Treatment of the purified, latent, D. salina CF1 with low concentrations of N-ethylmaleimide also results in the partial (approx. 60%) inhibition of the inducible ATPase activity (IC50 approximately 50 mM). N-ethylmaleimide-induced inhibition of the ATPase activity of either membrane-bound or solubilized CF1 is partially reversed by either prolonged incubation at low concentrations of N-ethylmaleimide or short incubation times at high concentrations of N-ethylmaleimide[4].
*该产品中的马来酰亚胺基团在碱性水溶液中会发生水解形成开环的马来酸酰胺衍生物,会影响生物学活性,例如无法和巯基形成共价硫醚键,影响和生物大分子的连接,建议现配现用,避免在水溶液中长期保存,可在中性或弱酸性水溶液中低温保存,反应时控制弱酸环境[5][6]

N-Ethylmaleimide/N-乙基马来酰亚胺 细胞实验

Cell Line
Concentration Treated Time Description References
Xenopus laevis oocytes 1 mM 10 minutes To investigate the inhibitory effect of NEM on hCAT-2A, it was found that NEM inhibits hCAT-2A activity by modifying Cys-33 and Cys-273. J Biol Chem. 2013 Oct 18;288(42):30411-30419.
CA1 pyramidal cells 250-300 µM 10-15 minutes To test the effect of NEM on G-protein-mediated DSI (depolarization-induced suppression of inhibition). NEM was found to block DSI and enhance GABA release. J Neurosci. 1997 Feb 1;17(3):941-50.
Immature cortical neurons 100 µM 15 minutes To investigate the effect of NEM on KCC2 activity in neurons, results showed that NEM significantly reduced intracellular Cl⁻ concentration. J Biol Chem. 2017 Dec 29;292(52):21253-21263.
HEK293 cells 100 µM 15 minutes To investigate the effect of NEM on KCC2 function, results showed that NEM significantly increased KCC2 transporter activity. J Biol Chem. 2017 Dec 29;292(52):21253-21263.

N-Ethylmaleimide/N-乙基马来酰亚胺 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Squid Squid giant presynaptic terminal Microinjection 0.05–2.5 mM Action potentials elicited every 1 s Inhibition of neurotransmitter release by photolysis of cNSF3 peptide, revealing the critical role of NSF in synaptic vesicle trafficking Proc Natl Acad Sci U S A. 2008 Jan 8;105(1):347-52

N-Ethylmaleimide/N-乙基马来酰亚胺 参考文献

[2]Wu KH, Tai PC. Cys32 and His105 are the critical residues for the calcium-dependent cysteine proteolytic activity of CvaB, an ATP-binding cassette transporter. J Biol Chem. 2004 Jan 9;279(2):901-9

[3]Specific inhibition of phosphate transport in mitochondria by N-ethylmaleimide

[4]Selman-Reimer S, Duhe RJ, Selman BR. N-Ethylmaleimide inhibition of the catalytic activities of the Dunaliella salina coupling factor 1 (CF1) and the restoration of the inhibition of the CF1 ATPase activity by N-ethylmaleimide. Biochim Biophys Acta. 1985 Dec 16;810(3):325-31

[5]Lyon RP, Setter JR, Bovee TD, Doronina SO, Hunter JH, Anderson ME, Balasubramanian CL, Duniho SM, Leiske CI, Li F, Senter PD. Self-hydrolyzing maleimides improve the stability and pharmacological properties of antibody-drug conjugates. Nat Biotechnol. 2014 Oct;32(10):1059-62.

[6]Knight P. Hydrolysis of p-NN'-phenylenebismaleimide and its adducts with cysteine. Implications for cross-linking of proteins. Biochem J. 1979 Apr 1;179(1):191-7.

N-Ethylmaleimide/N-乙基马来酰亚胺 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

7.99mL

1.60mL

0.80mL

39.96mL

7.99mL

4.00mL

79.92mL

15.98mL

7.99mL

N-Ethylmaleimide/N-乙基马来酰亚胺 技术信息

CAS号128-53-0
分子式C6H7NO2
分子量 125.13
SMILES Code O=C(N1CC)C=CC1=O
MDL No. MFCD00005509
别名 N-乙基顺丁烯二酰亚胺 ;NEM; NSC 7638
运输蓝冰
InChI Key HDFGOPSGAURCEO-UHFFFAOYSA-N
Pubchem ID 4362
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, 2-8°C

溶解方案

DMSO: 50 mg/mL(399.58 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 50 mg/mL(399.58 mM),配合低频超声助溶

无水乙醇: 12 mg/mL(95.9 mM),配合低频超声助溶,注意:无水乙醇开封后,易挥发,也会吸收空气中的水分,导致溶解能力下降,请避免使用开封较久的乙醇

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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
方案 一
方案 二
方案 三
配制的工作液建议现用现配,短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在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
方案 一
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