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APC-6860

Names

[ CAS No. ]:
154628-42-9

[ Name ]:
APC-6860

[Synonym ]:
1o5b
1c5n
1c5q
1c5x

Biological Activity

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C9H7IN2S

[ Molecular Weight ]:
302.13500

[ Exact Mass ]:
301.93700

[ PSA ]:
78.11000

[ LogP ]:
3.59000

Related Compounds