Dihydroeponemycin
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.
描述:抗增殖IC 50:100 nM [1]。
蛋白酶体是N-端亲核(Ntn)水解酶家族的成员,其氨基末端侧链可充当亲核体,游离氨基可作为质子受体。蛋白酶体抑制剂已被越来越多地用于帮助定义蛋白酶体在生物学中的作用。Dihydroeponemycin可标记免疫蛋白酶体亚基LMP2和LMP7,以及组成型蛋白酶体亚基X的催化苏氨酸残基,而epoxomicin(环氧酶素)可共价修饰组成型蛋白酶体(X和Z)以及免疫蛋白酶体(LMP7和MECL1)亚基的N端催化苏氨酸残基。
体外实验:以前的研究表明,抗肿瘤和抗血管生成的天然产物eponemycin的类似物dihydroeponemycin可选择性地靶向20S蛋白酶体。Dihydroeponemycin可共价修饰蛋白酶体催化亚基的一个子集,优先结合于IFN-γ诱导的LMP2和LMP7亚基。而且,dihydroeponemycin以不同的速率抑制蛋白酶体三个主要的多肽水解活性。Dihydroeponemycin介导的蛋白酶体的抑制可诱导纺锤状的细胞形态变化和细胞凋亡。这些结果验证了蛋白酶体可作为抗肿瘤药物干预的靶标,与新型化疗策略的设计相关[2]。
体内实验:在小鼠模型中,dihydrosterptomycin靶向毛细胞,因为在机械性感觉毛束中,氨基糖苷类可通过大型机械门控通道进入外毛细胞。氨基糖苷类分子进入后可阻断通道,因而可有效地将它们自己捕获在毛细胞中[3]。
临床试验:dihydrosterptomycin目前正处于临床前发展阶段。
参考文献:
[1] Kim KB, Myung J, Sin N, Crews CM. Proteasome inhibition by the natural products epoxomicin and dihydroeponemycin: insights into specificity and potency. Bioorg Med Chem Lett. 1999;9(23):3335-40.
[2] Meng L, Kwok BH, Sin N, Crews CM. Eponemycin exerts its antitumor effect through the inhibition of proteasome function. Cancer Res. 1999;59(12):2798-801.
[3] Marcotti W, van Netten SM, Kros CJ. The aminoglycoside antibiotic dihydrostreptomycin rapidly enters mouse outer hair cells through the mechano-electrical transducer channels. J Physiol. 2005;567(Pt 2):505-21.
Storage | Store at 2-8°C |
M.Wt | 400.51 |
Cas No. | 126463-64-7 |
Formula | C20H36N2O6 |
Synonyms | Dihydroeponemycin,uk101 |
Solubility | ≥15.6 mg/mL in DMSO |
Chemical Name | N-[(2S)-3-hydroxy-1-[[(2S)-1-[(2R)-2-(hydroxymethyl)oxiran-2-yl]-4-methyl-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]-6-methylheptanamide |
SDF | Download SDF |
Canonical SMILES | CC(C)CCCCC(=O)NC(CO)C(=O)NC(CC(C)C)C(=O)C1(CO1)CO |
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 |
牛主动脉内皮细胞 |
制备方法 |
可溶于DMSO。若配制更高浓度的溶液,一般步骤如下:请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。 |
反应条件 |
4 μM;0、12、24、36和48小时 |
实验结果 |
在牛主动脉内皮细胞中,95%细胞在Dihydroeponemycin处理的48小时中发生了DNA片段化。 |
References: [1]. Meng L, Kwok BH, Sin N, Crews CM. Eponemycin exerts its antitumor effect through the inhibition of proteasome function. Cancer Res. 1999;59(12):2798-801. |
描述 | Dihydroeponemycin是蛋白酶体的抑制剂和抗癌剂。 | |||||
靶点 | Proteasome | |||||
IC50 |
质量控制和MSDS
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