Table 1 Inhibitory activities of glycoconjugates 1, 2, 3a, 3b, 4a and 4b against ADAMTS-4 and -5.

From: Exosite inhibition of ADAMTS-5 by a glycoconjugated arylsulfonamide

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Compound

R

n

IC50 (μM)

ADAMTS-4

ADAMTS-5

1

0

40 ± 5

68 ± 6.5

3a

0

NI

NI

3b

0

50 ± 16

120 ± 20

2

1

51 ± 7.9

44 ± 8.9

4a

1

NI

NI

4b

1

NI

9.4 ± 2.8

  1. The inhibition of proteolysis was measured using the protein substrate V1-5GAG. NI, not inhibiting at 50 μM (< 10% inhibition compared with the DMSO controls). Values are presented as mean ± SEM (n = 3).
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