prolyl endopeptidase (IC50 = 6.3 μM)

N-乙基马来酰亚胺（20μM；30分钟）可防止Akt Ser-473、Akt Thr-308、p70S6K、核糖体蛋白S6、4E-BP1、eIF4E、BAD和FKHR-L1的磷酸化[2]
N-乙基马来酰亚胺（20μM；30分钟）影响血管平滑肌细胞中前天冬氨酸蛋白酶-3的转化[2]
N-乙基马来酰亚胺（20μM；6小时）诱导血管平滑肌细胞凋亡[2]
N-乙基马来酰亚胺（20μM；30分钟）对血管平滑肌细胞中的ROS产生和PP2A活性有影响[2]。

研究了辣椒素敏感感觉神经（CPSN）、内源性一氧化氮（NO）、巯基（SHs）、前列腺素（PGs）在苦瓜素Ic对大鼠乙醇诱导的胃黏膜损伤的胃保护作用中的作用。苦瓜苷Ic（10mg/kg，口服）可能抑制乙醇诱导的胃黏膜损伤。用辣椒素（总共125 mg/kg，皮下注射，CPSN的消融剂）、N（G）-硝基-L-精氨酸甲酯（L-NAME，70 mg/kg，腹腔注射，NO合酶抑制剂）、N-乙基马来酰亚胺（NEM，10 mg/kg，皮下接种，SH阻断剂）或吲哚美辛（10 mg/kg，静脉注射，PG生物合成抑制剂）预处理后，苦瓜素Ic的作用明显减弱。L-精氨酸（300mg/kg，静脉注射，NO合酶的底物）可消除L-NAME的衰减，但D-精氨酸却不能消除L-NAME衰减。辣椒素与吲哚美辛、NEM或L-NAME联合使用的效果并不比单独使用辣椒素强。吲哚美辛和NEM的组合、吲哚美辛和L-NAME的组合或吲哚美痛和NEM和L-NAME单独使用会增加每种药物的衰减。这些结果表明，CPSN在苦瓜素Ic对乙醇诱导的大鼠胃黏膜损伤的胃保护中起着重要作用，内源性PG、NO和SH相互作用。 [2]

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N-乙基马来酰亚胺（10 mg/kg；ih）会增加小鼠急性胃溃疡的患病率[3]。

在 Pierce IP 裂解缓冲液中制备细胞裂解物，其中含有蛋白酶抑制剂、磷酸酶抑制剂和去泛素化抑制剂 N-乙基马来酰亚胺（NEM，10mM），以促进内源蛋白免疫沉淀。首先将裂解物上清液与一抗在 4 °C 下孵育 14 小时，然后与 Dynabeads Protein G 磁珠结合并在 4 °C 下旋转 4 小时。使用磁力架分离磁珠-抗体复合物后，用PBST缓冲液洗涤磁珠3次。将复合物结合的珠子重悬于 1x 蛋白质电泳上样缓冲液中，并加热至 100°C 8 分钟，然后收集上清液进行 SDS-PAGE 分析。在制备用于外源蛋白免疫沉淀的细胞裂解物之前，将细胞转染 48 小时。同时使用抗小鼠 IgG 的抗体来制备阴性对照。

Male Sprague-Dawley rats
10 mg/kg
s.c.

Adverse Effects
Dermatotoxin - Skin burns.
Lacrimator (Lachrymator) - A substance that irritates the eyes and induces the flow of tears.
Toxic Pneumonitis - Inflammation of the lungs induced by inhalation of metal fumes or toxic gases and vapors.

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4362 rat LD50 oral 25 mg/kg BEHAVIORAL: SOMNOLENCE (GENERAL DEPRESSED ACTIVITY); BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD National Technical Information Service., OTS0536969
4362 rat LD50 intraperitoneal 1 mg/kg BEHAVIORAL: SOMNOLENCE (GENERAL DEPRESSED ACTIVITY) National Technical Information Service., OTS0536969
4362 rat LDLo intracrebral 1669 ug/kg Journal of Medicinal Chemistry., 15(534), 1972
4362 mouse LD50 oral 25 mg/kg BEHAVIORAL: SOMNOLENCE (GENERAL DEPRESSED ACTIVITY) National Technical Information Service., OTS0536969
4362 mouse LD50 intraperitoneal 5 mg/kg BEHAVIORAL: SOMNOLENCE (GENERAL DEPRESSED ACTIVITY) National Technical Information Service., OTS0536969

[1]. Cell Rep . 2022 Mar 22;38(12):110538.

[2]. Life Sci . 1999;65(2):PL27-32.

N-ethylmaleimide is a member of the class of maleimides that is the N-ethyl derivative of maleimide. It has a role as an EC 2.1.1.122 [(S)-tetrahydroprotoberberine N-methyltransferase] inhibitor, an EC 2.7.1.1 (hexokinase) inhibitor, an EC 1.3.1.8 [acyl-CoA dehydrogenase (NADP(+))] inhibitor and an anticoronaviral agent. It is functionally related to a maleimide.
A sulfhydryl reagent that is widely used in experimental biochemical studies.

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β-Catenin is a central component in the Wnt signaling pathway; its degradation has been tightly connected to ubiquitylation, but it is rarely examined by loss-of-function assays. Here we observe that endogenous β-catenin is not stabilized upon ubiquitylation depletion by a ubiquitylation inhibitor, TAK-243. We demonstrate that N-terminal phosphorylated β-catenin is quickly and strongly stabilized by a specific neddylation inhibitor, MLN4924, in all examined cell types, and that β-catenin and TCF4 interaction is strongly enhanced by inhibition of neddylation but not ubiquitylation. We also confirm that the E3 ligase β-TrCP2, but not β-TrCP1, is associated with neddylation and destruction of β-catenin. GSK3β and adenomatous polyposis coli (APC) are not required for β-catenin neddylation but essential for its subsequent degradation. Our findings not only clarify the process of β-catenin modification and degradation in the Wnt signaling pathway but also highlight the importance of reassessing previously identified ubiquitylation substrates. [1]

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The roles of capsaicin-sensitive sensory nerves (CPSN), endogenous nitric oxide (NO), sulfhydryls (SHs), prostaglandins (PGs) in the gastroprotection by momordin Ic, an oleanolic acid oligoglycoside isolated from the fruit of Kochia scoparia (L.) SCHRAD., on ethanol-induced gastric mucosal lesions were investigated in rats. Momordin Ic (10 mg/kg, p.o.) potentially inhibited ethanol-induced gastric mucosal lesions. The effect of momordin Ic was markedly attenuated by the pretreatment with capsaicin (125 mg/kg in total, s.c., an ablater of CPSN), N(G)-nitro-L-arginine methyl ester (L-NAME, 70 mg/kg, i.p., an inhibitor of NO synthase), N-ethylmaleimide (NEM, 10 mg/kg, s.c., a blocker of SHs), or indomethacin (10 mg/kg, s.c., an inhibitor of PGs biosynthesis). The attenuation of L-NAME was abolished by L-arginine (300 mg/kg, i.v., a substrate of NO synthase), but not by D-arginine (300 mg/kg, i.v., the enatiomer of L-arginine). The effect of the combination of capsaicin with indomethacin, NEM, or L-NAME was not more potent than that of capsaicin alone. The combination of indomethacin and NEM, indomethacin and L-NAME, or indomethacin and NEM and L-NAME increased the attenuation of each alone. These results suggest that CPSN play an important role in the gastroprotection by momordin Ic on ethanol-induced gastric mucosal lesions, and endogenous PGs, NO, and SHs interactively participate, in rats. [2]

C6H7NO2

125.13

125.047

C, 57.59; H, 5.64; N, 11.19; O, 25.57

128-53-0

N-Ethylmaleimide-d5;360768-37-2

4362

White to light yellow solid powder

1.2±0.1 g/cm3

210.0±9.0 °C at 760 mmHg

43-46 °C(lit.)

73.3±0.0 °C

0.2±0.4 mmHg at 25°C

1.514

0.68

37.38

0

2

1

9

166

0

O=C1C([H])=C([H])C(N1C([H])([H])C([H])([H])[H])=O

HDFGOPSGAURCEO-UHFFFAOYSA-N

InChI=1S/C6H7NO2/c1-2-7-5(8)3-4-6(7)9/h3-4H,2H2,1H3

1-ethylpyrrole-2,5-dione

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

注意： 本产品在运输和储存过程中需避光。

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

配方 1 中的溶解度: ≥ 2.08 mg/mL (16.62 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将100 μL 20.8 mg/mL澄清DMSO储备液加入400 μL PEG300中，混匀；然后向上述溶液中加入50 μL Tween-80，混匀；加入450 μL生理盐水定容至1 mL。
*生理盐水的制备：将 0.9 g 氯化钠溶解在 100 mL ddH₂O中，得到澄清溶液。

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配方 2 中的溶解度: ≥ 2.08 mg/mL (16.62 mM) (饱和度未知) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 20.8 mg/mL澄清DMSO储备液加入900 μL 20% SBE-β-CD生理盐水溶液中，混匀。
*20% SBE-β-CD 生理盐水溶液的制备（4°C，1 周）：将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中，得到澄清溶液。

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配方 3 中的溶解度: ≥ 2.08 mg/mL (16.62 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 20.8 mg/mL 澄清 DMSO 储备液加入到 900 μL 玉米油中并混合均匀。

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配方 4 中的溶解度: 100 mg/mL (799.17 mM) in PBS (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液; 超声助溶.

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。