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BRD4354 is a zinc chelating, reversible inhibitor of zinc-dependent histone deacetylases with selectivity for HDAC5 and HDAC9. BRD4354 has IC50 values of 0.85 μM and 1.88 μM for HDAC5 and HDAC9 respectively. Inhibition of other HDACs was lower, with IC50 values of 3.88-13.8 μM for HDACs 4, 6, 7, and 8 and over 40 μM for HDACs 1, 2, and 3. BRD4354′s mechanism is believed to involve zinc-catalyzed decomposition to an ortho-quinone methide, which covalently modifies nucleophilic cysteines within the proteins.
| Molecular Weight | 382.89 |
| Formula | C21H23ClN4O |
| CAS Number | 315698-07-8 |
| Solubility (25°C) | DMSO: 3 mg/mL (warmed) |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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