GGACK (H-Glu-Gly-Arg-chloromethylketone) 是一种不可逆的丝氨酸蛋白酶抑制剂，GGACK可抑制尿激酶型纤溶酶原激活剂（uPA）并阻断纤溶酶原激活过程。
Cas No.:65113-67-9
Sample solution is provided at 25 µL, 10mM.
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GGACK (H-Glu-Gly-Arg-chloromethylketone) is an irreversible serine protease inhibitor. GGACK can inhibit urokinase-type plasminogen activator (uPA) and block the plasminogen activation process. GGACK can be used for research related to cancer and coagulation-related diseases[1].
GGACK (10-100nM) had been used to treat PMA-stimulated U-937 leukemia cells for 30 minutes to induce high expression of uPAR, after which fluorescently labeled HMW-uPA was added. GGACK competitively inhibited the binding of HMW-uPA to the cell surface uPAR receptors[2].
References:
[1] Sperl S, Jacob U, Arroyo de Prada N, et al. (4-aminomethyl)phenylguanidine derivatives as nonpeptidic highly selective inhibitors of human urokinase. Proc Natl Acad Sci U S A. 2000 May 9;97(10):5113-8.
[2] De Souza M, Matthews H, Lee JA, et al. Small molecule antagonists of the urokinase (uPA): urokinase receptor (uPAR) interaction with high reported potencies show only weak effects in cell-based competition assays employing the native uPAR ligand. Bioorg Med Chem. 2011 Apr 15;19(8):2549-56.
GGACK (H-Glu-Gly-Arg-chloromethylketone) 是一种不可逆的丝氨酸蛋白酶抑制剂，GGACK可抑制尿激酶型纤溶酶原激活剂（uPA）并阻断纤溶酶原激活过程。GGACK可用于癌症和凝血相关疾病的相关研究[1]。
GGACK (10-100nM) 处理经PMA刺激以高表达uPAR的U-937白血病细胞30分钟，随后加入荧光标记的HMW-uPA，GGACK可竞争性抑制HMW-uPA与细胞表面uPAR受体的结合[2]。
| Cell experiment [1]: | |
Cell lines | U-937 cells (human monocyte-like leukemia cell line) |
Preparation Method | Phorbol 12-myristate-13-acetate (PMA)-stimulated U-937 cells were used. For the competition flow cytometry assay, cells were pre-incubated on ice for 30 minutes with 10nM or 100nM of either GGACK-inactivated HMW-uPA (i-uPA) or a test compound. Subsequently, 1nM of Alexa Fluor 488-labeled active HMW-uPA was added and incubated with the cells for 30 minutes on ice. The samples were then washed, fixed, and analyzed by flow cytometry. |
Reaction Conditions | 10nM or 100nM; 30min pre-incubation on ice. |
Applications | GGACK-inactivated HMW-uPA (i-uPA) potently antagonized the binding of Alexa Fluor 488-labeled active HMW-uPA to cell surface urokinase-type plasminogen activator receptors (uPAR). GGACK inhibited the fluorescent signal, demonstrating its strong efficacy as a competitive antagonist in the uPA:uPAR binding assay. |
References: | |
| Cas No. | 65113-67-9 | SDF | |
| 别名 | 精氨酸杂质 | ||
| 分子式 | C14H25ClN6O5 | 分子量 | 392.84 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5456 mL | 12.7278 mL | 25.4557 mL |
| 5 mM | 509.1 μL | 2.5456 mL | 5.0911 mL |
| 10 mM | 254.6 μL | 1.2728 mL | 2.5456 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
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