APC-6860 (hydrochloride) 

APC-6860 hydrochloride is a competitive, selective arylamidine Serine protease inhibitor, with a K_i of 0.44 μM for trypsin, 0.10 μM for h-uPA, and 0.082 μM for mouse uPA. APC-6860 hydrochloride inhibits urokinase-activated plasminogen-mediated degradation of Fibronectin in cancer cells. APC-6860 hydrochloride is applicable to research related to breast cancer and prostate cancer^[1][2].

APC-6860 hydrochloride potently and competitively inhibits uPA with a K_i 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) hydrochloride exhibits inhibitory activity against h-urokinase, with a K_i value of 0.10 μM^[2].
APC-6860 (0.01-250 μM) hydrochloride inhibits recombinant murine urokinase, with a K_i value of 0.082 μM^[2].
APC-6860 (serial dilution; 2.5 h) hydrochloride 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) hydrochloride 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.

338.60

C₉H₈ClIN₂S

149732-36-5

IC1=CC=CC2=C1C=C(C(N)=N)S2.Cl

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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]