Benzo[b]thiophene-2-carboximidamide, 4-iodo-

APC-6860 is a trypsin-like serine proteases inhibitor with ki values of 0.21 and 0.44 μM for uPA and trypsin, respectively. APC-6860 has a selectivity ratio for tPA versus uPA of 80. APC-6860 has ki values of 0.1 and 0.082 μM for human and murine urokinases, respectively. APC-6860 can be used for the research of cancer[1][2].

uPA: 0.21 μM (Ki); trypsin: 0.44 μM (Ki); tryptase: 1.5 μM (Ki); tPA: 16.8 μM (Ki); thrombin: 20 μM (Ki); factor Xa: 30 μM (Ki); human urokinases: 0.1 μM (Ki); murine urokinases: 0.082 μM (Ki)

[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. DOI:10.1016/s1074-5521(00)00104-6
[2] Klinghofer V, et al. Species specificity of amidine-based urokinase inhibitors. Biochemistry. 2001 Aug 7;40(31):9125-31. DOI:10.1021/bi010186u