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Cathepsin G Inhibitor I
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Cathepsin G Inhibitor I图片
CAS NO:429676-93-7
包装与价格:
包装价格(元)
500ug电议
1mg电议
5mg电议

产品介绍

化学性质

Physical AppearanceA solid
StorageStore at -20°C
M.Wt620.64
Cas No.429676-93-7
FormulaC36H33N2O6P
Solubility≥10.35 mg/mL in DMSO
Chemical Name[2-[3-[(1-benzoylpiperidin-4-yl)-methylcarbamoyl]naphthalen-2-yl]-1-naphthalen-1-yl-2-oxoethyl]phosphonic acid
Canonical SMILESCN(C1CCN(CC1)C(=O)C2=CC=CC=C2)C(=O)C3=CC4=CC=CC=C4C=C3C(=O)C(C5=CC=CC6=CC=CC=C65)P(=O)(O)O
运输条件蓝冰运输或根据您的需求运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。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。

资料参考

Cathepsin G(EC 3.4.21.20、胰凝乳酶样蛋白酶、中性蛋白酶)是一种酶蛋白,属于肽酶或蛋白酶家族。在人类中,它由CTSG基因编码。Cathepsin G Inhibitor I是一种有效的、选择性的、可逆的和竞争性的非肽类cathepsin G抑制剂。

体外实验:Cathepsin G Inhibitor I可逆并竞争性地抑制cathepsin G,IC50和Ki值分别为53 ± 12 nM(n = 10)和63 ± 14 nM(n = 5)。与其它丝氨酸蛋白酶相比,Cathepsin G Inhibitor I对cathepsin G具有选择性,对糜蛋白酶作用较弱(Ki = 1.5 ± 0.2 μM),对凝血酶、因子Xa、因子IXa、纤溶酶、胰蛋白酶、类胰蛋白酶、蛋白酶3和人白细胞弹性蛋白酶的抑制作用极弱(在100μM时具有<50%的抑制)[1]。

体内试验:Cathepsin G Inhibitor I目前正用于体外研究,没有相关的动物实验[1]。

临床试验:Cathepsin G Inhibitor I目前处于临床前开发阶段,没有相关的临床试验[1]。

参考文献:
[1] Greco MN, Hawkins MJ, Powell ET, Almond HR Jr, Corcoran TW, de Garavilla L, Kauffman JA, Recacha R, Chattopadhyay D, Andrade-Gordon P, Maryanoff BE.  Nonpeptide inhibitors of cathepsin G: optimization of a novel beta-ketophosphonic acid lead by structure-based drug design. J Am Chem Soc. 2002;124(15):3810-1.

试验操作

Cell experiment:[1]

Cell lines

Metastatic breast cancer cells and neutrophils

Reaction Conditions

2 μM cathepsin G inhibitor I for 22 h incubation

Applications

Cathepsin G inhibitor I (2 μM) reduced the formation of neutrophil extracellular traps (NETs) induced by cancer cells. In addition, cathepsin G inhibitor I (2 μM) inhibited neutrophil-stimulated invasion. Thus, inhibition of cathepsin G, a protease associated with NETs, was able to reduce the extension of NETs and block neutrophils’ ability to promote invasion.

Note

The technical data provided above is for reference only.

References:

1. Park J, Wysocki RW, Amoozgar Z, et al. Cancer cells induce metastasis-supporting neutrophil extracellular DNA traps. Science Translational Medicine, 2016, 8(361): 361ra138.

生物活性

Cathepsin G Inhibitor I是一种有效的、选择性的和竞争性的非肽类cathepsin G抑制剂。.
靶点cathepsins G     
IC5053nM