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Merck
CN

474790

MG-132

≥98% (HPLC), proteasome inhibitor, solid

别名:

Z-Leu-Leu-Leu-al, MG-132

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关于此项目

经验公式（希尔记法）:
C26H41N3O5
化学文摘社编号:
133407-82-6
分子量:
475.62
MDL编号:
MFCD00674886
UNSPSC代码:
12352200
NACRES:
NA.77

主要文件

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产品名称

MG-132, A cell-permeable, potent, reversible proteasome inhibitor (Ki = 4 nM).

质量水平

100

方案

≥98% (HPLC)

表单

solid

制造商/商品名称

Calbiochem®

储存条件

OK to freeze

颜色

white

溶解性

DMSO: 20 mg/mL
ethanol: 20 mg/mL

运输

ambient

储存温度

−20°C

SMILES字符串

[H]C(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)OCc1ccccc1

InChI

1S/C26H41N3O5/c1-17(2)12-21(15-30)27-24(31)22(13-18(3)4)28-25(32)23(14-19(5)6)29-26(33)34-16-20-10-8-7-9-11-20/h7-11,15,17-19,21-23H,12-14,16H2,1-6H3,(H,27,31)(H,28,32)(H,29,33)/t21-,22-,23-/m0/s1

InChI key

TZYWCYJVHRLUCT-VABKMULXSA-N

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相关类别

Amino Acid Sequence

Z-Leu-Leu-Leu-al

一般描述

高效、可逆和细胞可透过性蛋白酶体抑制剂（(Ki = 4 nM）。可通过26S复合物降低哺乳动物细胞和酵母可渗透菌株中泛素结合蛋白的降解，而不会影响其ATP酶或异肽酶的活性。可激活c-Jun N端激酶（JNK1），从而启动细胞凋亡。抑制NF-κB的活化（IC50 = 3 µM）。也有报道称，间充质干细胞移植后的存活率增加。防止β-分泌酶裂解。也可购买10 mM（1 mg/210 µl）MG-132 DMSO溶液（货号474791）。HPLC法测定该物质纯度≥98%。另提供经HPLC测试为≥95%纯度产品（货号474787）。

生化/生理作用

4 nM抗蛋白酶体
主要靶标
蛋白酶体
产品不与ATP竞争。
可逆性：是
细胞渗透性：是
靶标IC50：3 µM抑制NF-κB活化

制备说明

溶解后，等分并冷冻保存（-20°C）。储备溶液在-20°C下可稳定保存1个月。

其他说明

Li, Z.W. et al. 2011.Sheng Li Xue Bao.63, 525.
Steinhilb, M.L., et al. 2001.J. Biol. Chem.276, 4476.
Meriin, A.B., et al. 1998.J. Biol. Chem. 273, 6373.
Adams, J., and Stein, R. 1996.Ann.Rep.Med. Chem.31, 279.
Klafki, H.W., et al. 1996.J. Biol. Chem.271, 2865.
Lee, D.H., and Goldberg, A.L., 1996.J. Biol. Chem.271, 27280.
Wiertz, E.J., et al. 1996.Cell84, 769.
Jensen, T.J., et al. 1995.Cell 83, 129.
Read, M.A., et al. 1995.
Cell 78, 761.
Z-Leu-Leu-Leu-CHO

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

免责声明

毒性：标准处理（A）

储存分类代码

11 - Combustible Solids

WGK

WGK 3

分析证书(COA)

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Monika Chauhan et al.
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It is critical for the neuronal cell cycle to remain suppressed in terminally differentiated neurons as its activation results in aberrant cell cycle re-entry that causes neuronal apoptosis (CRNA), which has been observed in several neurodegenerative disorders like Alzheimer's disease
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Nucleic acids research, 48(1), 486-499 (2019-11-21)
Cross-species pathway transplantation enables insight into a biological process not possible through traditional approaches. We replaced the enzymes catalyzing the entire Saccharomyces cerevisiae adenine de novo biosynthesis pathway with the human pathway. While the 'humanized' yeast grew in the absence
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Proceedings of the National Academy of Sciences of the United States of America, 118(4) (2021-01-23)
The reversibility of ubiquitination by the action of deubiquitinating enzymes (DUBs) serves as an important regulatory layer within the ubiquitin system. Approximately 100 DUBs are encoded by the human genome, and many have been implicated with pathologies, including neurodegeneration and
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Nonalcoholic fatty liver disease (NAFLD) and nonalcoholic steatohepatitis (NASH) are emerging as leading causes of liver disease worldwide and have been recognized as one of the major unmet medical needs of the 21st century. Our recent translational studies in mouse
Katarzyna A Ludwik et al.
Cell reports, 32(3), 107931-107931 (2020-07-23)
In response to estrogens, estrogen receptor alpha (ERα), a critical regulator of homeostasis, is degraded through the 26S proteasome. However, despite the continued presence of estrogen before menopause, ERα protein levels are maintained. We discovered that ERK1/2-RSK2 activity oscillates during
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