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. 2022 Dec 15;299(1):102800. doi: 10.1016/j.jbc.2022.102800

Table 2.

Kinetic parameters of the inhibition of HDAC6 by 1

HDAC6 forms Parameters 1
Human HDAC6 IC50, nM 7.7 ± 0.3
8.1 ± 0.3a
konapp, M−1 min−1 (×105)b 9.6 ± 0.3
9.1 ± 0.3a
koffapp, min−1 (×10−3)b 4.6 ± 2.3
6.7 ± 1.9a
koffapp, min−1 (×10−3)c 3.3 ± 0.2
Kiapp, nMd 4.8 ± 2.4
6.9 ± 1.9a
Mode of inhibition Slow-on/slow-off
zHDAC6-CD2 WT IC50, nM 7.8 ± 0.4
konapp, M−1 min−1 (×105)b 15.1 ± 0.1
koffapp, min−1 (×10−3)b 12.8 ± 1.1
koffapp, min−1 (×10−3)c 9.6 ± 1.1
Kiapp, nMd 8.5 ± 0.7
Mode of inhibition Slow-on/slow-off
zHDAC6-CD2 Y745F IC50, nM 15.1 ± 0.9
konapp, M−1 min−1 (×105)b ∼1010d
koffapp, min−1 (×10−3)c 92.7 ± 3.2
Mode of inhibition Fast-on/slow-off
a

Parameters determined in D2O.

b

Calculated from kobs plot, Kiapp = koffapp/konapp.

c

koffapp values from jump-dilution assay.

d

Parameter estimated from koffapp/Kiapp ratio.