Chemical Structure : BRD4884
CAS No.: 1404559-91-6
Catalog No.: PC-72672Not For Human Use, Lab Use Only.
BRD4884 is a potent, kinetically selective HDAC2 inhibitor with IC50 of 29/62 nM for HDAC1/2, >17-fold selectivity versus HDAC3.
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BRD4884 is a potent, kinetically selective HDAC2 inhibitor with IC50 of 29/62 nM for HDAC1/2, >17-fold selectivity versus HDAC3.
BRD4884 shows slow-on/slow-off kinetics for HDAC2, but a shift to fast-on/faster-off kinetics for HDAC1, leading to a 7-fold longer half-life on HDAC2 (T 1/2 143 min) versus HDAC1 (T 1/2 20 min). This binding profile provides kinetic selectivity for HDAC2 and good thermodynamic selectivity for HDAC1, 2 versus HDAC3.
BRD4884 produced significant increases in AcH4K12 and AcH3K9 in mouse forebrain primary neuronal cultures.
BRD4884 (10 mg/kg) rescued the memory defects associated with p25 induced neurodegeneration in a murine model of neurodegeneration.
M.Wt | 314.4 | |
Formula | C18H19FN2O2 | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
N-(4-amino-4'-fluoro[1,1'-biphenyl]-3-yl)tetrahydro-2H-pyran-4-carboxamide |
1. F F Wagner, et al. Chem Sci. 2015 Jan 1;6(1):804-815.
2. Wagner FF, et al. Bioorg Med Chem. 2016 Sep 15;24(18):4008-4015.
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