HAT inhibitor / Potent and selective inhibitor of the histone acetyl transferase p300/CBP (Ki=400 nM ). Induces apoptosis in prostate cancer cells. Enhances fear extinction memory and synaptic plasticity in mice. Promotes tau deacetylation reducing levels of pathogenic p-tau. Cell permeable.
Biochemicals & reagents
328968-36-1
Bowers et al. (2010), Virtual ligand screening of the p300/CBP histone acetyltransferase: identification of a selective small molecule inhibitor; Chem. Biol., 17 471 / 2) Santer et al. (2011), Inhibition of the acetyltransferases p300 and CBP reveals a targetable function for p300 in the survival and invasion pathways of prostate cancer cell lines; Mol. Cancer Ther., 10 1644 / 3) Marek et al. (2011), Paradoxical enhancement of fear extinction memory and synaptic plasticity by inhibition of the histone acetyltransferase p300; J. Neurosci.., 31 7486 / 4) Min et al. (2010), Acetylation of tau inhibits its degradation and contributes to tauopathy; Neuron, 67 953
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TARGET: Acetyltransferase -- PATHWAY: Chromatin; Posttranslational modification; Apoptosis inducer; Transcription -- RESEARCH AREA: Epigenetics; Cell death; Neuroscience -- DISEASE AREA: Cancer; Neurodegeneration