CAS NO: | 429676-93-7 |
包装 | 价格(元) |
500ug | 电议 |
1mg | 电议 |
5mg | 电议 |
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 620.64 |
Cas No. | 429676-93-7 |
Formula | C36H33N2O6P |
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 SMILES | CN(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。 |
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.
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. |
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 | |||||
IC50 | 53nM |