Epoxomicin
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Epoxomicin(环氧酶素)对小鼠B16黑色素瘤具有抗肿瘤活性,最初是从放线菌菌株的培养基中分离得到的。Epoxomicin是一种天然存在的选择性蛋白酶体抑制剂,具有抗炎活性[1]。Epoxomicin主要抑制胰凝乳蛋白酶样蛋白酶体(CTRL)的活性。
Epoxomicin的α-环氧酮可以与酶特定催化亚基中的残基形成共价键,从而抑制其活性。Epoxomicin也可以抑制蛋白酶体的胰蛋白酶样活性和肽基谷氨酰基肽(peptidyl-glutamyl peptide)水解活性,比对CTRL的抑制速率慢100倍和1000倍。泛素 - 蛋白酶体途径很大程度上可以调节骨形成,从而Epoxomicin可以增加啮齿类动物中骨的体积和骨形成的速率。
另一项研究表明,Epoxomicin和其它的蛋白酶体抑制剂可以导致多巴胺能细胞死亡,从而产生帕金森病(Parkinson's disease)的体内模型。Epoxomicin是20S蛋白酶体的抑制剂。
参考文献:
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.
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Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 554.7 |
Cas No. | 134381-21-8 |
Formula | C28H50N4O7 |
Synonyms | Epoxomicin, BU4061T, BU-4061T |
Solubility | ≥27.73 mg/mL in DMSO; insoluble in H2O; ≥77.4 mg/mL in EtOH |
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 |
SDF | Download SDF |
Canonical SMILES | CCC(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 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 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。溶液形式一般不宜长期储存,请尽快用完。 |
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. |
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 |
质量控制和MSDS
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