Uses
PCI-34051 is a potent, histone deacetylase 8 (HDAC8)-specific inhibitor. PCI-34051 induces caspase-dependent apoptosis in cell lines derived from T-cell lymphomas or leukemias. PCI-34051 did not affect other hematopoietic or solid tumor lines. PCI-34051 treatment has been shown to significantly reduce cholesterol accumulation in Niemann-Pick type C1 gene mutated human fibroblast.
Biological Activity
pci-34051 is a potent, specific inhibitor of histone deacetylase 8 (hdac8) with greater than 200-fold selectivity over the other hdac isoforms, such as 1, 2, 3, 6 and 10. it induces caspase dependent apoptosis in cell lines derived from t-cell lymphomas or leukemias, but not in other hematopoietic or solid tumor lines. pci-34051 does not cause detectable histone or tubulin acetylation and also does not inhibit growth or induce apoptosis in normal cells such as pbmcs or fibroblasts. although a phospholipase c-gamma1 (plcgamma1) defective line is resistant, cells defective in t-cell receptor signaling are still sensitive to pci-34051 induced apoptosis.