APC-6860

Modify Date: 2024-01-09 16:52:01

APC-6860 Structure
APC-6860 structure
Common Name APC-6860
CAS Number 154628-42-9 Molecular Weight 302.13500
Density N/A Boiling Point N/A
Molecular Formula C9H7IN2S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of APC-6860


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].

 Names

Name 4-iodo-1-benzothiophene-2-carboximidamide
Synonym More Synonyms

 APC-6860 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
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

 Synonyms

1o5b
1c5n
1c5q
1c5x
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