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B-苄氧羰基-亮氨酸-亮氨酸-正缬氨酸

B-苄氧羰基-亮氨酸-亮氨酸-正缬氨酸用途

MG-115是一种有效的可逆蛋白酶体抑制剂,其Kis分别为21nm和35nm,用于20S和26S蛋白酶体。MG-115特异性抑制蛋白酶体的糜蛋白酶样活性,诱导p53依赖性凋亡[1][2][3]。

B-苄氧羰基-亮氨酸-亮氨酸-正缬氨酸名称

[ CAS 号 ]:
133407-86-0

[ 中文名 ]:
MG115,蛋白酶体抑制剂

[ 英文名 ]:
MG-115

[英文别名 ]:

MG115 Z-LLnV

B-苄氧羰基-亮氨酸-亮氨酸-正缬氨酸生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 细胞凋亡 >> 细胞凋亡

研究领域 >> 癌症

信号通路 >> 代谢酶/蛋白酶 >> 蛋白酶体

[ 靶点 ]

Ki: 21 nM (20S proteasome); 35 nM (26 Sproteasome)[1]

[体外研究]

MG-115(0.1-10μM；24小时)剂量依赖性地降低HepG2细胞的活力[3]。MG-115(0.1-10μM；24小时)放大了CWK18 DNA凝聚物介导的报告基因表达[3]。细胞活力测定[3]细胞系：HepG2细胞浓度：0.1,1,2,5,10μM培养时间：24小时结果：细胞活力呈剂量依赖性降低。抑制蛋白酶体活性,IC50为2 μM。

[参考文献]

[1]. Rock KL, et, al. Inhibitors of the proteasome block the degradation of most cell proteins and the generation of peptides presented on MHC class I molecules. Cell. 1994 Sep 9;78(5):761-71.

[2]. Lopes UG, et, al. p53-dependent induction of apoptosis by proteasome inhibitors. J Biol Chem. 1997 May 16;272(20):12893-6.

[3]. Kim J, et, al. The proteasome metabolizes peptide-mediated nonviral gene delivery systems. Gene Ther. 2005 Nov;12(21):1581-90.

B-苄氧羰基-亮氨酸-亮氨酸-正缬氨酸物理化学性质

[ 密度 ]:
1.1±0.1 g/cm3

[ 沸点 ]:
678.8±55.0 °C at 760 mmHg

[ 分子式 ]:
C₂₅H₃₉N₃O₅

[ 分子量 ]:
461.59

[ 闪点 ]:
364.3±31.5 °C

[ 精确质量 ]:
461.288971

[ PSA ]:
113.60000

[ LogP ]:
5.41

[ 外观性状 ]:
白色粉末

[ 蒸汽压 ]:
0.0±2.1 mmHg at 25°C

[ 折射率 ]:
1.508

[ 储存条件 ]:
室温，干燥，密封

B-苄氧羰基-亮氨酸-亮氨酸-正缬氨酸MSDS

详细MSDS(安全技术说明书)

B-苄氧羰基-亮氨酸-亮氨酸-正缬氨酸安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危险品运输编码 ]:
NONH for all modes of transport

B-苄氧羰基-亮氨酸-亮氨酸-正缬氨酸文献

Development of two novel high-throughput assays to quantify ubiquitylated proteins in cell lysates: application to screening of new anti-malarials.

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3,4,5-tricaffeoylquinic acid attenuates proteasome inhibition-mediated programmed cell death in differentiated PC12 cells.

Neurochem. Res. 39(8) , 1416-25, (2014)

The dysfunction of the proteasome system is suggested to be implicated in neuronal degeneration. Caffeoylquinic acid derivatives have demonstrated anti-oxidant and anti-inflammatory effects. However, ...

HEMERA Couples the Proteolysis and Transcriptional Activity of PHYTOCHROME INTERACTING FACTORs in Arabidopsis Photomorphogenesis.

Plant Cell 27 , 1409-27, (2015)

Phytochromes (phys) are red and far-red photoreceptors that control plant development and growth by promoting the proteolysis of a family of antagonistically acting basic helix-loop-helix transcriptio...

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