Cathepsin G Inhibitor I
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
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.
| 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 |
| SDF | Download SDF |
| 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 | 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。 |
| Cell experiment:[1] | |
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Cell lines |
Metastatic breast cancer cells and neutrophils |
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Reaction Conditions |
2 μM cathepsin G inhibitor I for 22 h incubation |
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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. |
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Note |
The technical data provided above is for reference only. |
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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. |
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| 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 | |||||
质量控制和MSDS
- 批次：
化学结构
