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MG-115

现货
Catalog No.
A2612
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)
¥ 1,400.00
现货
5mg
¥ 700.00
现货
25mg
¥ 2,000.00
现货
100mg
¥ 7,000.00
现货

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Background

MG-115 (Z-Leu-Leu-Nva-H) is a potent, reversible peptide aldehyde inhibitor of proteasome chymotrypsin-like and caspase-like activities. It induces p53 dependent apoptosis. Blockade of proteasomal degradation by MG115 can activate autophagy.

Treatment with proteasome inhibitors Z-Leu-Leu-Nva-H (MG-115) or Z-Leu-Leu-Leu-H (MG-132) prevented the accelerated degradation of these mutant receptors, resulting in increased amounts of the mutant receptors in the COS-7 cells [1].

A potent, reversible proteasome inhibitor with Ki of 21 nM for 20S proteasome and 35 nM for 26S proteasome. The inhibition of proteasome was through specific inhibition of chymotrypsin-like activity of the proteasome. Also shown to induce apoptosis in Rat-1 and PC12 cells via a p3-independent pathway.

References:
1. Involvement of heat shock protein 90 in the degradation of mutant insulin receptors by the proteasome. Imamura, T., Haruta, T., Takata, Y., Usui, I., Iwata, M., Ishihara, H., Ishiki, M., Ishibashi, O., Ueno, E., Sasaoka, T., Kobayashi, M. J. Biol. Chem. (1998)

文献引用

1. Wang Y, Lu S, et al. "Sonic hedgehog induces GLT-1 degradation via PKC delta to suppress its transporter activities." Neuroscience. 2017 Oct 6;365:217-225. PMID:28993237

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
该产品在溶液中不稳定,建议现配现用
M.Wt461.59
Cas No.133407-86-0
FormulaC25H39N3O5
SynonymsCarbobenzoxy-L-leucyl-L-leucyl-L-norvalinal, Z-LL-Nva-CHO, Proteasome Inhibitor XII,MG115
Solubility≥23.1mg/mL in DMSO
Chemical Namebenzyl N-[(2S)-4-methyl-1-[[(2S)-4-methyl-1-oxo-1-[[(2S)-1-oxopentan-2-yl]amino]pentan-2-yl]amino]-1-oxopentan-2-yl]carbamate
SDFDownload SDF
Canonical SMILESCCCC(C=O)NC(=O)C(CC(C)C)NC(=O)C(CC(C)C)NC(=O)OCC1=CC=CC=C1
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

表达突变型或野生型胰岛素受体的转染COS-7细胞

制备方法

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℃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℃可放置数月。

反应条件

50 μM;2小时

实验结果

在Leu1193和Asp1179突变细胞系中,MG-115使胰岛素受体及其成熟β亚基的表达分别增加3倍和4.2倍。然而,在野生型细胞系中,两者表达没有发生变化。结果表明,Leu1193和Asp1179突变胰岛素受体通过细胞质中的蛋白酶体降解。

References:

[1]. Imamura T, Haruta T, Takata Y, et al. Involvement of heat shock protein 90 in the degradation of mutant insulin receptors by the proteasome. J Biol Chem, 1998, 273(18): 11183-11188.

质量控制

化学结构

MG-115

相关生物数据

MG-115

相关生物数据

MG-115

相关生物数据

MG-115