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Merck
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文件

474790

Sigma-Aldrich

MG-132

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

别名:

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

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About This Item

经验公式(希尔记法):
C26H41N3O5
分子量:
475.62
MDL编号:
UNSPSC代码:
12352200
NACRES:
NA.77

质量水平

检测方案

≥98% (HPLC)

形式

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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Amino Acid Sequence

Z-Leu-Leu-Leu-al

一般描述

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-kB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。
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。µ号474791)的DMSO溶液。HPLC法测定该物质纯度≥98%。一种物质,HPLC法测定的纯度≥95%(目录。

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

警告

毒性:标准处理(A)

序列

Z-Leu-Leu-Leu-CHO

重悬

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.

法律信息

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

WGK

WGK 3


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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
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Molecular & cellular proteomics : MCP, 19(9), 1450-1467 (2020-06-20)
Insulin receptor substrate 2 (IRS2) is an essential adaptor that mediates signaling downstream of the insulin receptor and other receptor tyrosine kinases. Transduction through IRS2-dependent pathways is important for coordinating metabolic homeostasis, and dysregulation of IRS2 causes systemic insulin signaling

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