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Epoxomicin

现货
Catalog No.
A2606
蛋白酶体抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 5,000.00
现货
1mg
¥ 1,350.00
现货
5mg
¥ 4,000.00
现货
20mg
¥ 12,000.00
现货

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Background

Epoxomicin was originally isolated from the culture medium of an Actinomycetes strain based on its in vivo antitumor activity against murine B16 melanoma. Epoxomicin is a naturally occurring selective proteasome inhibitor with anti-inflammatory activity. [1] Epoxomicin primarily inhibits the activity of CTRL (chymotrypsin-like proteasome).

The novel α-epoxy ketone moiety of Epoxomicin forms covalent bonds with residues in particular catalytic subunits of the enzyme, disabling activity. The trypsin-like and peptidyl-glutamyl peptide hydrolyzing behaviors of the proteasome were both inhibited by Epoxomicin as well (at 100 and 1,000-fold slower rates, respectively). The ubiquitin-proteasome pathway heavily regulates bone formation, and Epoxomicin was shown to increase both bone volume and bone formation rates in rodents.

Another study demonstrates that exposure to Epoxomicin and other proteasome inhibitors leads to dopaminergic cell death, producing a model of Parkinson's disease in vivo. Epoxomicin is an inhibitor of 20S Proteasome. [2]

References:
1. Meng, L; Mohan, R; Kwok, BH; Elofsson, M; Sin, N; Crews, CM (1999). "Epoxomicin, a potent and selective proteasome inhibitor, exhibits in vivo antiinflammatory activity". PNAS 96 (18): 10403–10408.
2. Epoxomicin, Santa Cruz Biotechnology.

文献引用

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt554.7
Cas No.134381-21-8
FormulaC28H50N4O7
SynonymsEpoxomicin,BU4061T,BU-4061T
Solubility≥27.74mg/mL in DMSO
Chemical Name(2S,3S)-2-[[(2S,3S)-2-[acetyl(methyl)amino]-3-methylpentanoyl]amino]-N-[(2S,3R)-3-hydroxy-1-[[(2S)-4-methyl-1-[(2R)-2-methyloxiran-2-yl]-1-oxopentan-2-yl]amino]-1-oxobutan-2-yl]-3-methylpentanamide
SDFDownload SDF
Canonical SMILESCCC(C)C(C(=O)NC(C(C)O)C(=O)NC(CC(C)C)C(=O)C1(CO1)C)NC(=O)C(C(C)CC)N(C)C(=O)C
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验[1]:

细胞系

HEK293T细胞

溶解方法

在DMSO中的溶解度>10 mM。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应条件

0.2 μM / 2 μM;1 h

应用

多肽可以被来自细胞质、线粒体和核蛋白的蛋白酶体降解。Epoxomicin是一种蛋白酶体抑制剂。在HEK293T细胞中,epoxomicin可以降低细胞内大部分多肽的水平,同时抑制蛋白酶体beta-2和beta-5亚基。

动物实验[2]:

动物模型

C57BL6小鼠

剂量

Epoxomicin(0.58 mg/kg)溶解于10% DMSO/PBS中,腹腔注射(i.p.),6天。

应用

Epoxomicin减少三硝基氯苯(picrylchloride)诱导的炎症。在刺激后的24小时进行耳廓肿胀测试,epoxomicin有效抑制95%的刺激相关的炎症反应。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。

References:

1. Fricker LD1, Gelman JS, Castro LM et al. Peptidomic analysis of HEK293T cells: effect of the proteasome inhibitor epoxomicin on intracellular peptides. J Proteome Res. 2012 Mar 2;11(3):1981-90.

2. Meng L1, Mohan R, Kwok BH et al. Epoxomicin, a potent and selective proteasome inhibitor, exhibits in vivo antiinflammatory activity. Proc Natl Acad Sci U S A. 1999 Aug 31;96(18):10403-8.

生物活性

描述 Epoxomicin是选择性的和不可逆的蛋白酶体抑制剂,IC50值为4 nM。
靶点 20S proteasome          
IC50 4 nM          

质量控制

化学结构

Epoxomicin

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