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]。