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]
Technical information:
| Chemical Formula: | C17H16N2O3 | |
| CAS #: | 950762-95-5 | |
| Molecular Weight: | 296.32 | |
| Purity: > 99% | ||
| Appearance: | White | |
| Chemical Name: | 1-(4-methoxybenzyl)-N-hydroxy-1H-indole-6-carboxamide | |
| Solubility: | Up to 100 mM in DMSO | |
| Synonyms: | PCI-34051, PCI34051 |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | Balasubramanian et al., A novel histone deacetylase 8 (HDAC8)-specific inhibitor PCI-34051 induces apoptosis in T-cell lymphomas, Leukemia, 2008, 22(5), 1026-1034. Pubmed ID: 18256683 |
| 2. | Pipalia et al., Histone deacetylase inhibitor treatment dramatically reduces cholesterol accumulation in Niemann-Pick type C1 mutant human fibroblasts. Proc. Nat. Acad. Sci. 2011, 108(14), 5620-5625. Pubmed ID: 21436030 |
Other Information:
Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.
