Table 2.
Biochemical characterization of dual inhibitors against LSD1 and HDAC1 as part of the CoREST ternary complex
| 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 |
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)
aDash marks indicate that compound was not evaluated in the corresponding assay. Data (mean ± SEM) are representative of at least two independent experiments