APC-6860
APC-6860 is a competitive, selective arylamidine Serine protease inhibitor, with a Ki of 0.44 μM for trypsin, 0.10 μM for h-uPA, and 0.082 μM for mouse uPA. APC-6860 inhibits urokinase-activated plasminogen-mediated degradation of Fibronectin in cancer cells. APC-6860 is applicable to research related to breast cancer and prostate cancer.
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- CAS. Nr.: 154628-42-9
- Formel: C9H7IN2S
- Molecular Weight:302.13
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
Beschreibung
In Vitro
APC-6860 potently and competitively inhibits uPA with a Ki value of 0.21 µM. It exhibits low inhibitory activity against trypsin-like serine proteases including trypsin, tryptase, tPA, thrombin and factor Xa, and shows 80-fold higher selectivity for uPA over tPA[1].
APC-6860 (Compound 2) (0.01-250 μM) exhibits inhibitory activity against h-urokinase, with a Ki value of 0.10 μM[2].
APC-6860 (0.01-250 μM) inhibits recombinant murine urokinase, with a Ki value of 0.082 μM[2].
APC-6860 (serial dilution; 2.5 h) inhibits urokinase-mediated fibronectin degradation in MiaPaCa-2 pancreatic cancer cells with an IC50 of 1.4 μM[2].
APC-6860 (serial dilution; 2.5 h) inhibits urokinase-mediated fibronectin degradation in mouse Lewis lung cancer cells, with an IC50 of 3.1 μM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 154628-42-9
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Molecular Weight 302.13
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Formel C9H7IN2S
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SMILES
N=C(C1=CC2=C(I)C=CC=C2S1)N
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[1]. Katz BA, et al. Structural basis for selectivity of a small molecule, S1-binding, submicromolar inhibitor of urokinase-type plasminogen activator. Chem Biol. 2000 Apr;7(4):299-312. [Content Brief]
[2]. Klinghofer V, et al. Species specificity of amidine-based urokinase inhibitors. Biochemistry. 2001;40(31):9125-9131. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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