PCI-34051 | HDAC 8 inhibitor

PCI-34051 (950762-95-5) is a potent and selective HDAC8 inhibitor (IC₅₀=10 nM) with greater than 200-fold selectivity over HDACs 1, 2, 3, 6, 10.¹ Unlike broad-spectrum HDAC inhibitors, it does not cause detectable histone or tubulin acetylation.¹  Studies employing PCI-34051 showed that HDAC8 catalyzes the hydrolysis of long chain fatty acyl lysine.² It is a very useful tool for exploring the role of HDAC8 in cellular function.^3-6

References/Citations:

1. Balasubramanian et al. (2008), A novel histone deacetylase 8 (HDAC8)-specific inhibitor PCI-34051 induces apoptosis in T-cell lymphomas; Leukemia 22 1026
2. Aramsangtienchai et al. (2016), HDAC8 Catalyzes the Hydrolysis of Long Chain Fatty Acyl Lysine; ACS Chem. Biol. 11 2685
3. Dasgupta et al. (2016), HDAC8 Inhibition Blocks SMC3 Deacetylation and Delays Cell Cycle Progression without Affecting Cohesion-dependent Transcription in MCF7 Cancer Cells; J. Biol. Chem. 291 12761
4. Ha et al. (2016), Inhibition of Interleukin 1ß (IL-1ß) Expression by Anthrax Lethal Toxin (LeTx) is Reversed by Histone Deacetylase 8 (HDAC8) Inhibition in Murine Macrophages; J. Biol. Chem. 291 8745
5. Fukuda et al. (2024), Inhibition of HDAC8 Reduces the Proliferation of Adult Neural Stem Cells in the Subventricular Zone; Int. J. Mol. Sci. 25 2540
6. Mormino et al. (2024), Histone-deacetylase 8 drives the immune response and the growth of glioma; Glia 69 2682