Molecular structure of uPA Inhibitor, CAS Number: 149732-36-5
uPA Inhibitor Inhibitor (CAS 149732-36-5)
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Alternate Names:
4-iodo-1-benzothiophene-2-carboximidamide hydrochloride
Application:
uPA Inhibitor is a substrate-competetive inhibitor of uPA, trypsin, and tryptase
CAS Number:
149732-36-5
Molecular Weight:
338.6
Molecular Formula:
C9H7IN2S•HCl
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
uPA Inhibitor is a cell-permeable carboxamidine compound reported to act as a potent, substrate-competitive inhibitor of uPA (Ki = 0.32μM), trypsin (Ki = 0.44 μM), and tryptase (Ki = 1.5 µM). This compound is also reported to have good selectivity relative to tPA, Thrombin, and Factor Xa. Additionally reported to block cell surface uPA-mediated, plasminogen-dependent degradation of fibronectin by HT1080 cells in a dose-dependent manner (IC50 = 540 nM).
uPA Inhibitor Inhibitor (CAS 149732-36-5) References
- Structural basis for selectivity of a small molecule, S1-binding, submicromolar inhibitor of urokinase-type plasminogen activator. | Katz, BA., et al. 2000. Chem Biol. 7: 299-312. PMID: 10779411
- Urokinase-type plasminogen activator: a potent marker of metastatic potential in human cancers. | Duffy, MJ. 2002. Biochem Soc Trans. 30: 207-10. PMID: 12023852
- Urokinase-type plasminogen activator (uPA) and its inhibitor PAI-I: novel tumor-derived factors with a high prognostic and predictive impact in breast cancer. | Harbeck, N., et al. 2004. Thromb Haemost. 91: 450-6. PMID: 14983219
- Dissecting and designing inhibitor selectivity determinants at the S1 site using an artificial Ala190 protease (Ala190 uPA). | Katz, BA., et al. 2004. J Mol Biol. 344: 527-47. PMID: 15522303
- Identification of a novel inhibitor of urokinase-type plasminogen activator. | Zhu, M., et al. 2007. Mol Cancer Ther. 6: 1348-56. PMID: 17431113
- Breast cancer and metabolic syndrome linked through the plasminogen activator inhibitor-1 cycle. | Beaulieu, LM., et al. 2007. Bioessays. 29: 1029-38. PMID: 17876797
- Urokinase plasminogen activator and its inhibitor type-1 as prognostic factors in differentiated thyroid carcinoma patients. | Horvatic Herceg, G., et al. 2013. Otolaryngol Head Neck Surg. 149: 533-40. PMID: 23835563
- The many spaces of uPAR: delivery of theranostic agents and nanobins to multiple tumor compartments through a single target. | O'Halloran, TV., et al. 2013. Theranostics. 3: 496-506. PMID: 23843897
- Synthesis and in vivo preclinical evaluation of an (18)F labeled uPA inhibitor as a potential PET imaging agent. | Ides, J., et al. 2014. Nucl Med Biol. 41: 477-87. PMID: 24768145
- Structural Principles in the Development of Cyclic Peptidic Enzyme Inhibitors. | Xu, P., et al. 2017. Int J Biol Sci. 13: 1222-1233. PMID: 29104489
- Discovery of selective urokinase plasminogen activator (uPA) inhibitors as a potential treatment for multiple sclerosis. | Islam, I., et al. 2018. Bioorg Med Chem Lett. 28: 3372-3375. PMID: 30201291
- Disruption of Water Networks is the Cause of Human/Mouse Species Selectivity in Urokinase Plasminogen Activator (uPA) Inhibitors Derived from Hexamethylene Amiloride (HMA). | S El Salamouni, N., et al. 2022. J Med Chem. 65: 1933-1945. PMID: 34898192
- The synthesis of three 4-substituted benzo[b]thiophene-2-carboxamidines as potent and selective inhibitors of urokinase. | Bridges, AJ., et al. 1993. Bioorg Med Chem. 1: 403-10. PMID: 8087561
- Inhibition of urokinase by 4-substituted benzo[b]thiophene-2-carboxamidines: an important new class of selective synthetic urokinase inhibitor. | Towle, MJ., et al. 1993. Cancer Res. 53: 2553-9. PMID: 8495419
- Prevention of prostate-cancer metastasis in vivo by a novel synthetic inhibitor of urokinase-type plasminogen activator (uPA). | Rabbani, SA., et al. 1995. Int J Cancer. 63: 840-5. PMID: 8847143
Inhibitor of:
Protease, tPA, Trypsin, Tryptase, and uPA.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
uPA Inhibitor, 5 mg | sc-356184 | 5 mg | $311.00 |