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. 2021 Jan 13;11:949. doi: 10.1038/s41598-020-80294-1

Table 1.

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

graphic file with name 41598_2020_80294_Figa_HTML.gif
Compound R n IC50 (μM)
ADAMTS-4 ADAMTS-5
1 graphic file with name 41598_2020_80294_Figb_HTML.gif 0 40 ± 5 68 ± 6.5
3a graphic file with name 41598_2020_80294_Figc_HTML.gif 0 NI NI
3b graphic file with name 41598_2020_80294_Figd_HTML.gif 0 50 ± 16 120 ± 20
2 graphic file with name 41598_2020_80294_Fige_HTML.gif 1 51 ± 7.9 44 ± 8.9
4a graphic file with name 41598_2020_80294_Figf_HTML.gif 1 NI NI
4b graphic file with name 41598_2020_80294_Figg_HTML.gif 1 NI 9.4 ± 2.8

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).