GGACK (H-Glu-Gly-Arg-chloromethylketone) |
Katalog-Nr.GA22381
One-Click Copy Product Info
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GGACK (EGR-CMK), Hemmer des u-Plasminogenaktivators. Unumkehrbarer kovalenter Inhibitor von menschlichem Hepsin.
Products are for research use only. Not for human use. We do not sell to patients.
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.
| 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 | |
| Formula | C14H25ClN6O5 | M.Wt | 392.84 |
| Löslichkeit | Soluble in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 25 reference(s) in Google Scholar.)