Table 1 The IC50 of HDAC family inhibition of bisthianostat in vitro.

From: Pharmacodynamic, pharmacokinetic, and phase 1a study of bisthianostat, a novel histone deacetylase inhibitor, for the treatment of relapsed or refractory multiple myeloma

HDAC

IC50 (μM)

BIS

SAHA

HDAC1

0.095 ± 0.049

0.211 ± 0.114

HDAC2

0.193 ± 0.065

0.474 ± 0.142

HDAC3

0.108 ± 0.060

0.232 ± 0.147

HDAC4

0.158 ± 0.048

0.354 ± 0.126

HDAC5

0.138 ± 0.051

0.311 ± 0.092

HDAC6

0.068 ± 0.030

0.180 ± 0.086

HDAC7

>20

>20

HDAC8

0.221 ± 0.136

0.415 ± 0.233

HDAC9

>20

>20

HDAC10

0.171 ± 0.094

0.410 ± 0.242

HDAC11

0.141 ± 0.023

0.609 ± 0.580

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