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PCI-34051 is a potent and selective inhibitor of HDAC8 with >200-fold selectivity over the other HDAC isoforms 1, 2, 3, 6 and 10 with IC50 values of 4, >50, >50, 2.9 and 13 μM, respectively. PCI-34051 induces caspase-dependent apoptosis in cell lines derived from T-cell lymphomas or leukemias (GI50s = 2.4 - 4 μM), but not in other hematopoietic or solid tumor lines. PCI-34051 does not cause detectable histone or tubulin acetylation like other broad-spectrum HDAC inhibitors. PCI-34051-induced apoptosis upon treatment with a PLC inhibitor U73122 showed a dose-dependent decrease on Jurkat cells. The mechanism by which PCI-34051 induces apoptosis in T-cell lines is also novel to the histone deacetylase field; it involves Ca2+ signaling via phospholipase C-gamma1.
University of Otago. 2019.
Transcriptional effects of mood stabiliser drugs in a serotonergic cell line
PCI-34051 purchased from AbMole
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Source | J Biol Chem (2016). Figure 1. PCI-34051 |
| Method | immunoblotting | |
| Cell Lines | MCF7 cells | |
| Concentrations | 10 μM | |
| Incubation Time | 48 h | |
| Results | At both time points and at all concentrations, PCI-34051 caused an accumulation of acetylated SMC3 compared with vehicle controls, whereas total SMC3 remained unchanged. |
| Molecular Weight | 296.32 |
| Formula | C17H16N2O3 |
| CAS Number | 950762-95-5 |
| Solubility (25°C) | DMSO 49 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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