MG-115
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.
MG-115（Z-Leu-Leu-Nva-H）是一种有效的和可逆的肽醛类蛋白酶体糜蛋白酶样和caspase样活性抑制剂。MG-115诱导p53依赖的细胞凋亡，其对蛋白酶体降解的阻断可激活自体吞噬。
在COS-7细胞中，用蛋白酶体抑制剂Z-Leu-Leu-Nva-H（MG-115）或Z-Leu-Leu-Leu-H（MG-132）处理可防止突变受体的加速降解，从而导致突变受体的数量增加[1]。
MG-115是一种有效的和可逆的蛋白酶体抑制剂，作用于20S蛋白酶体和26S蛋白酶体，Ki值分别为21 nM和35 nM。对蛋白酶体的抑制是通过特异性抑制蛋白酶体的糜蛋白酶样活性。在Rat-1和PC12细胞中，MG-115诱导p53依赖的细胞凋亡。
参考文献：
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)
- 1. Abhishesh Bajracharya, Jing Xi, et al. "PHYTOCHROME-INTERACTING FACTOR 4/HEMERA-mediated thermosensory growth requires the Mediator subunit MED14." Plant Physiol. 2022 Nov 28;190(4):2706-2721. PMID: 36063057
- 2. 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
| Physical Appearance | A solid |
| Storage | Store at -20°C该产品在溶液中不稳定，建议现配现用 |
| M.Wt | 461.59 |
| Cas No. | 133407-86-0 |
| Formula | C25H39N3O5 |
| Synonyms | Carbobenzoxy-L-leucyl-L-leucyl-L-norvalinal, Z-LL-Nva-CHO, Proteasome Inhibitor XII,MG115 |
| Solubility | ≥23.08 mg/mL in DMSO; insoluble in H2O; ≥26.5 mg/mL in EtOH |
| Chemical Name | benzyl 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 |
| SDF | Download SDF |
| Canonical SMILES | CCCC(C=O)NC(=O)C(CC(C)C)NC(=O)C(CC(C)C)NC(=O)OCC1=CC=CC=C1 |
| 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 |
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. |
|
质量控制和MSDS
- 批次：
化学结构
相关生物数据
相关生物数据
相关生物数据
