HDAC3 selective inhibitor / Potent and selective HDAC3 inhibitor (IC50 = 289 nM), IC50s for HDAC1, 2 and 6 = 2, 2.2 and >20 mM respectively.1 Inhibits tumor growth in a mouse xenograft model of human multiple myeloma.1 Downregulates expression of DNA methyltransferase 1.2 Increases expression of synaptic proteins in exogenous Aβ-treated cells and mice.3 Rescues synaptic damage and neuron loss in APP-transfected cells (15 mM) and APP/PS1 mice (30 mg/kg).4
Biochemicals & reagents
926259-99-6
1 Minami et al. (2014), Histone deacetylase 3 as a novel therapeutic target in multiple myeloma; Leukemia, 28 680 2 Harada et al. (2017), HDAC3 regulates DNMT1 expression in multiple myeloma: therapeutic implications; Leukemia, 31 2670 3 Han et al. (2021), Class I HDAC Inhibitor Improves Synaptic Proteins and Repairs Cytoskeleton Through Regulating Synapse-Related Genes In vitro and In vivo; Front. Aging Neurosci., 12 619866 4 Han et al. (2022), A Class I HDAC Inhibitor Rescues Synaptic Damage and Neuron Loss in APP-Transfected Cells and APP/PS1 Mice through the GRIP1/AMPA Pathway; Molecules, 27 4160
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TARGET: Protein deacetylase -- PATHWAY: Myc; Posttranslational modification -- RESEARCH AREA: Epigenetics; Neuroscience -- DISEASE AREA: Neurodegeneration; Cancer