Table 2 Biochemical characterization of dual inhibitors against LSD1 and HDAC1 as part of the CoREST ternary complex

From: Targeting the CoREST complex with dual histone deacetylase and demethylase inhibitors

Cmpd ID

CoREST complex (LSD1) IC50 (µM)

CoREST complex (HDAC1) IC50 (µM)

1

1.8 ± 0.3

0.230 ± 0.014

2 (corin)

0.33 ± 0.05

0.206 ± 0.035

bizine

1.4 ± 0.6

ND

GSK2879552a

0.38 ± 0.01

–

7

0.36 ± 0.01

ND

9

 > 20

0.328 ± 0.026

  1. LSD1 assay: CoREST complex = 100 nM, substrate = 60 µM dimethyl histone H3K41–21 peptide; HDAC1 assay: CoREST complex = 2 nM, substrate = 50 µM acetylated P53379–382 tetrapeptide RHKK(Ac)
  2. aDash marks indicate that compound was not evaluated in the corresponding assay. Data (mean ± SEM) are representative of at least two independent experiments
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