MG-115
英文名称: MG-115
型号:null    产品货号: IUP1017-0001MG
价格:请致电:010-57128832,18610462672
品牌: gene operation

 IUP1017-MG-115

MG-115≥95%

【英文同义名】:Z-LLnV, Z-LL-Nva-CHO, Z-leu-leu-norvalinal

【中文同义名】:

订购信息:(原装进口,常备现货)

 

产品名称

产品货号

目录价(元)

Gene Operation

MG-115 (Proteasome inhibitor)

IUP1017-0001MG

1MG

989.00

IUP1017-0005MG

5MG

2439.00

产品描述

MG-115(同义名: Z-LLnV, Z-LL-Nva-CHO, Z-leu-leu-norvalinal) 是一种强效的,可逆的肽醛类蛋白酶体(proteasome)抑制剂,抑制20S26S蛋白酶体的Ki分别是 21nM 35nM[1-2]MG-115还能特异性抑制蛋白酶体的类糜蛋白酶活性,并且通过p53依赖途径诱导Rat-1PC12细胞凋亡[3]

靶点

靶点

20S proteasome

26S proteasome

IC50(半数有效浓度)

21 nM(Ki)

35 nM(Ki)

化学特性

Cas No.: 133407-86-0

分子量: 461.6

分子式: C25H39N3O5

纯度: ≥95% 

同义名: Z-LLnV, Z-LL-Nva-CHO, Z-leu-leu-norvalinal

化学名: Carbobenzoxy-L-leucyl-L-leucyl-L-norvalinal

外观: 白色至类白色粉末

溶解: 溶于DMSO(up to 50 mg/mL)

保存:3 -20 粉末

储存液配制

储存液 (1 ml DMSO体系)

1 mM

5 mM

10 mM

25 mM

50 mM

质量(mg)

0.4616

2.3080

4.6160

11.5400

23.0800

结构式

使用浓度(仅作参考)

MG-115的具体使用浓度请参考相关文献,并根据自身实验条件(如实验目的,细胞种类,培养特性等)进行摸索和优化。

参考文献

[1] Vinitsky A, et al. Inhibition of the chymotrypsin-like activity of the pituitary multicatalytic proteinase complex. Biochemistry. 31(39):9421-8 (1992).

[2] Palombella VJ, et al. The ubiquitin-proteasome pathway is required for processing the NF- kappa B1 precursor protein and the activation of NF-kappa B. Cell. 78(5):773-85 (1994).

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

US" style="font-size:10.0pt;font-family:"Arial",sans-serif;mso-bidi-font-weight:bold">Thapsigargin的具体使用浓度请参考相关文献,并根据自身实验条件(如实验目的,细胞种类,培养特性等)进行摸索和优化。

参考文献

[1] Hakii H., et al. Thapsigargin, a histamine secretagogue, is a non-12-O-tetradecanolphorbol-

13- acetate (TPA) type tumor promoter in two-stage mouse skin carcinogenesis. J Cancer Res Clin Oncol. 111 (3): 177–81 (1986).

[2] Davidson GA, et al. Kinetics of thapsigargin-Ca(2+)-ATPase (sarcoplasmic reticulum) inter- action reveals a two-step binding mechanism and picomolar inhibition. J Biol Chem. 270(20): 11731-4 (1995).

[3] Thastrup O, et al. Thapsigargin, a novel molecular probe for studying intracellular calcium release and storage. Agents Actions. 27(1-2):17-23 (1989).

[4] Inesi G, et al. Thapsigargin, a high affinity and global inhibitor of intracellular Ca2+ transport ATPases. Arch Biochem Biophys. 98(2):313-7 (1992).

[5] Treiman M, et al. A tool coming of age: thapsigargin as an inhibitor of sarco-endoplasmic reticulum Ca(2+)-ATPases. Trends Pharmacol Sci. 19(4):131-5 (1998).

[6] Jackisch C, et al. Delayed micromolar elevation in intracellular calcium precedes induction of apoptosis in thapsigargin-treated breast cancer cells. Clin Cancer Res. 6(7):2844-50 (2000).

[7] Ding WX, et al. Differential effects of endoplasmic reticulum stress-induced autophagy on cell survival. J Biol Chem. 282(7):4702-10 (2007).