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
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 |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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