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

Table 2.

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

graphic file with name 41598_2020_80294_Figh_HTML.gif
Compound R1 R2 IC50 (μM)
QF peptide		 IC50 (μM)
V1-5GAG
ATS4 ATS5 ATS4 ATS5
4b graphic file with name 41598_2020_80294_Figi_HTML.gif graphic file with name 41598_2020_80294_Figj_HTML.gif NIa NIa NIb 9.4 ± 2.8
4c graphic file with name 41598_2020_80294_Figk_HTML.gif graphic file with name 41598_2020_80294_Figl_HTML.gif NIa 57 ± 10 90 ± 44 62 ± 12
4d graphic file with name 41598_2020_80294_Figm_HTML.gif graphic file with name 41598_2020_80294_Fign_HTML.gif NIa NI 180 ± 50 90 ± 23
5b graphic file with name 41598_2020_80294_Figo_HTML.gif graphic file with name 41598_2020_80294_Figp_HTML.gif NIa NIa 30% inhibition at 100 μM NIb
6 graphic file with name 41598_2020_80294_Figq_HTML.gif graphic file with name 41598_2020_80294_Figr_HTML.gif NIa NIa NIb NIb

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).