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BRD73954 does not only retained HDAC6 inhibitory activity (IC50 = 0.036 μM) but resulted in a 10-fold increase in potency for HDAC8 (IC50 = 0.12 μM) with a concomitant reduction in potency for HDAC2.
In vitro: While treatment BRD73954 with resulted in a robust increase in α-tubulin acetylation, no change in the acetylation state of H3 was observed, which is consistent with the ability of these compounds to inhibit HDAC6 but not HDACs 1, 2, or 3 in the biochemical assay in HeLa cells.
| Molecular Weight | 284.31 |
| Formula | C16H16N2O3 |
| CAS Number | 1440209-96-0 |
| Solubility (25°C) | DMSO 30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[1] Olson DE, et al. J Med Chem. Discovery of the first histone deacetylase 6/8 dual inhibitors.
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