PCI 34051

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.

Definition

ChEBI: N-hydroxy-1-[(4-methoxyphenyl)methyl]-6-indolecarboxamide is an indolecarboxamide.

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.

in vivo

IC 50

HDAC8: 10 nM (IC₅₀); HDAC6: 2.9 μM (IC₅₀); HDAC1: 4 μM (IC₅₀); HDAC10: 13 μM (IC₅₀)

storage

-20°C