Garcinol
HAT inhibitor / Garcinol is a HAT (histone acetyltransferase) inhibitor (p300 IC50=7µM and PCAF IC50=5µM) both in vitro and in vivo.1 It potentiates TRAIL-induced apoptosis of cancer cells. Garcinol, independent of the cell type, induces both of the TRAIL receptors, death receptor 4 (DR4) and DR5. Garcinol neither induces the receptors of normal cells nor sensitizes them to TRAIL.2
Biochemicals & reagents
78824-30-3
1) Balasubramanyam, et al.; (2004) Polyisoprenylated benzophenone, garcinol, a natural histone acetyltransferase inhibitor, represses chromatin transcription and alters global gene expression J. Biol. Chem. 279 33716 / 2) Prasad, et al. (2010) Garcinol potentiates TRAIL-induced apoptosis through modulation of death receptors and antiapoptotic proteins Mol. Cancer Ther. 9, 856
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TARGET: Acetyltransferase -- PATHWAY: Chromatin; Apoptosis inducer; Posttranslational modification -- RESEARCH AREA: Epigenetics; Cell death; Stem cells