Table 2 Inhibitory activities of 4b and its derivatives, 4c, 4d, 5b and 6, against ADAMTS-4 and -5.

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

Compound

R1

R2

IC50 (μM)

QF peptide

IC50 (μM)

V1-5GAG

ATS4

ATS5

ATS4

ATS5

4b

NIa

NIa

NIb

9.4 ± 2.8

4c

NIa

57 ± 10

90 ± 44

62 ± 12

4d

NIa

NI

180 ± 50

90 ± 23

5b

NIa

NIa

30% inhibition at 100 μM

NIb

6

NIa

NIa

NIb

NIb

  1. The inhibition of proteolysis was measured using either a short, 12-residue, peptide substrate (QF-peptide) or the protein substrate V1-5GAG. Values are presented as mean ± SEM (n = 3). ATS4, ADAMTS-4; ATS5, ADAMTS-5. NIa, not inhibiting at 50 μM. NIb, not inhibiting at 100 μM (< 10% inhibition compared with the DMSO controls).
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