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. Author manuscript; available in PMC: 2020 Jan 15.
Published in final edited form as: Bioorg Med Chem Lett. 2018 Nov 28;29(2):204–211. doi: 10.1016/j.bmcl.2018.11.055

Table 2.

Kinetic parameters for the inhibition of recombinant USP7 catalytic domain (USP7CD) and USP9x.

Cmpd USP7CD USP9x
kon
(M−1 s−1)
kon
(M−1 s−1)
C14 13 ± 4 18 ± 2
C15 8 ± 3 6 ± 1
C17 9 ± 4 49 ± 3
C18 NI 17 ± 1
C20 21 ± 2 NI
C22 NI 58 ± 3
WP1130 66 ± 4 50 ± 30
b-AP15 n.d. 140 ± 10
PR619 n.d. 90 ± 20
D12 prost n.d. NI
BITC a n.d. 170 ± 40
PEITC a n.d. 150 ± 20

Data were fit to a single step inactivation mechanism as described in Material and Methods. NI, no inhibition; n.d., not determined. The values of kon for benzylisothiocyanate (BEITC) and phenethylisothiocyante (PEITC) are included for comparison.

a.

Values from 13.