PCI-34051
| CAS No. | 950762-95-5 | Cat. No. | BCP03674 |
| Name | PCI-34051 | ||
| Synonyms | PCI34051; PCI 34051; | ||
| Formula | C17H16N2O3 | M. Wt | 296.32 |
| Description | IC50 Value: 10 nM HDAC8-selective inhibitor,PCI-34051, has a unique mechanism of action involving PLCgamma1 activation and calcium-induced apoptosis, and could offer benefits including a greater therapeutic index for treating T-cell malignancies. in vitro: PCI-34051 is a specific inhibitor of HDAC8 with >200-fold selectivity over the other HDAC isoforms.PCI-34051 induces caspase-dependent apoptosis in cell lines derived from T-cell lymphomas or leukemias, but not in other hematopoietic or solid tumor lines. Unlike broad-spectrum HDAC inhibitors, PCI-34051 does not cause detectable histone or tubulin acetylation. Cells defective in T-cell receptor signaling were still sensitive to PCI-34051-induced apoptosis, whereas a phospholipase C-gamma1 (PLCgamma1)-defective line was resistant. HDAC8-inhibitor specifically induces cell death in T-cell-derived lines, which is caspase dependent | ||
| Pathways | Cell Cycle/DNA Damage Epigenetics | ||
| Targets | HDAC | ||
Structure
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