154628-42-9

154628-42-9 structure

Name: APC-6860
Chemical Name: 4-iodo-1-benzothiophene-2-carboximidamide
CAS Number: 154628-42-9
Molecular Formula: C₉H₇IN₂S
Molecular Weight: 302.13500
Catalog: Signaling Pathways Metabolic Enzyme/Protease Ser/Thr Protease
Create Date: 2016-01-20 06:02:00
Modify Date: 2025-08-25 16:03:41
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].

Name	4-iodo-1-benzothiophene-2-carboximidamide
Synonyms	1o5b 1c5n 1c5q 1c5x

Description	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].
Related Catalog	Signaling Pathways >> Metabolic Enzyme/Protease >> Ser/Thr Protease Research Areas >> Cancer
Target	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)
In Vitro	APC-6860 (compound 2) inhibits urokinases in MiaPaCa-2 and Lewis Lung Carcinoma cells with IC50s of 1.4 and 3.1 μM, respectively[2].
References	[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. [2]. Klinghofer V, et al. Species specificity of amidine-based urokinase inhibitors. Biochemistry. 2001 Aug 7;40(31):9125-31.