PCI-34051 is a indole-based hydroxamic acid inhibitor of HDAC-8 with an IC50 of 10 nM. It is at least 200-fold selective over other HDAC isoforms with micromolar IC50s of 4, >50, >50, 2.9, and 13 for HDAC-1, HDAC-2, HDAC-3, HDAC-6, and HDAC-10. [1] PCI-34051 induces caspase-dependent apoptosis at low micromolar concentrations in cell lines derived from T-cell lymphomas, including Jurkat and HuT78, but is not cytotoxic to other hematopoietic or solid tumor lines. Unlike other unselective or pan-HDAC inhibitors, PCI-34051 does not induce histone or tubulin acetylation.

The unique specificity of PCI-34051 was used to invalidate HDAC-8 as a potential target for reduction or cholesterol accumulation in lysosomal storage organelles (LSOs) of two NPC1 mutant human fibroblast lines. [2]

PCI-34051 is a indole-based hydroxamic acid inhibitor of HDAC-8 with an IC50 of 10 nM. It is at least 200-fold selective over other HDAC isoforms with micromolar IC50s of 4, >50, >50, 2.9, and 13 for HDAC-1, HDAC-2, HDAC-3, HDAC-6, and HDAC-10. [1] PCI-34051 induces caspase-dependent apoptosis at low micromolar concentrations in cell lines derived from T-cell lymphomas, including Jurkat and HuT78, but is not cytotoxic to other hematopoietic or solid tumor lines. Unlike other unselective or pan-HDAC inhibitors, PCI-34051 does not induce histone or tubulin acetylation.

The unique specificity of PCI-34051 was used to invalidate HDAC-8 as a potential target for reduction or cholesterol accumulation in lysosomal storage organelles (LSOs) of two NPC1 mutant human fibroblast lines. [2]