PCI-24781 is a novel hydroxamic acid HDAC inhibitor (histone deacetylase inhibitor). ?PCI-24781 exerts cytotoxicity and histone H3 alterations via caspase-8 and FADD in leukemia cells.
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This broad-spectrum histone deacetylase inhibitor (FW = 394.48 g/mol; CASs = 783355-60-2, 783356-67-2 (HCl)); Solubility: 80 mg/mL DMSO; <1 mg/mL Water; Formulated in 30% HP-cyclodextrin in water), also known as CRA-024781 and systematically as 3-((dimethylamino)methyl)- N-(2-(4-(hydroxycarbamoyl)phenoxy)ethyl)benzofuran-2-carboxamide, is a novel broad-spectrum HDAC inhibitor targeting HDAC1, HDAC2, HDAC3, HDAC6, HDAC8 and HDAC10 with Ki of 7 nM, 19 nM, 8.2 nM, 17 nM, 280 nM, 24 nM, respectively. PCI-24781 treatment causes dosedependent accumulation of both acetylated histones and acetylated tubulin in HCT116 or DLD-1 cells. It also induces expression of p21 and leads to PARP cleavage and accumulation of the γH2AX.
