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PCI-34051

Cat. No. M2101

PCI-34051 Structure
Size Price Availability Quantity
10mg USD 115 In stock
50mg USD 450 In stock
100mg USD 756 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 296.32
Formula C17H16N2O3
CAS Number 950762-95-5
Purity >99%
Solubility DMSO 50 mg/mL
Storage at -20°C
References

A novel histone deacetylase 8 (HDAC8)-specific inhibitor PCI-34051 induces apoptosis in T-cell lymphomas.
Balasubramanian S, et al. Leukemia. 2008 May;22(5):1026-34. PMID: 18256683.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: PCI-34051 supplier, HDAC, inhibitors

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