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PCI-34051

Cat. No. M2101
PCI-34051 Structure
Size Price Availability Quantity
5mg USD 61  USD61 In stock
10mg USD 108  USD108 In stock
25mg USD 218  USD218 In stock
50mg USD 416  USD416 In stock
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Quality Control & Documentation
Biological Activity

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.

Product Citations
Customer Product Validations & Biological Datas
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.
Chemical Information
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
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Balasubramanian S, et al. Leukemia. A novel histone deacetylase 8 (HDAC8)-specific inhibitor PCI-34051 induces apoptosis in T-cell lymphomas.

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Keywords: PCI-34051 supplier, HDAC, inhibitors, activators


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