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    PCI-34051
    PCI-34051

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0279
    CAS #: 950762-95-5Purity ≥98%

    Description: PCI-34051 is a novel, potent and specific inhibitor of  histone deacetylase 8 (HDAC8) with potential anticancer activity. It inhibits HDAC8 with an IC50 of 10 nM in a cell-free assay, and shows >200-fold selectivity for HDAC8 over HDAC1 and 6, and 1000-fold higher selectivity over HDAC2/3/10.

    References: Leukemia. 2008 May;22(5):1026-34.

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    Molecular Weight (MW)296.32
    FormulaC17H16N2O3
    CAS No.950762-95-5
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 59 mg/mL (199.1 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo)30% PEG400+0.5% Tween80+5% propylene glycol: 30mg/mL
    Synonyms

    PCI-34051; PCI 34051; PCI34051

    Chemical Name: N-hydroxy-1-(4-methoxybenzyl)-1H-indole-6-carboxamide

    InChi Key: AJRGHIGYPXNABY-UHFFFAOYSA-N

    InChi Code: InChI=1S/C17H16N2O3/c1-22-15-6-2-12(3-7-15)11-19-9-8-13-4-5-14(10-16(13)19)17(20)18-21/h2-10,21H,11H2,1H3,(H,18,20)

    SMILES Code: O=C(C1=CC2=C(C=C1)C=CN2CC3=CC=C(OC)C=C3)NO 


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    In Vitro

    In vitro activity: PCI-34051 possesses promising potency for HDAC8 with a Ki of 10 nM. PCI-34051 has high selectivity (approximately fivefold) for HDAC8 relative to the other class I HDACs including HDAC1. PCI-34051 reveals greater than 200-fold selectivity over HDAC1 and HDAC6, and greater than 1000-fold selectivity over HDAC2, HDAC3 and HDAC10. PCI-34051 inhibits ovarian tumor line OVCAR-3 with a GI50 of 6 μM and 15% cell death. Neither significant tubulin nor histone acetylation is observed in the sensitive cell lines treated with PCI-34051 at concentrations less than 25 μM at 24 hours nor at earlier timepoints. PCI-34051 induces a selective cytotoxic effect in cell lines derived only from T-cell malignancies. PCI-34051 induces caspase-dependent apoptosis. When caspase-3 activity is measured at various times after treatment with 5 μM PCI-34051, increasing levels of activity are observed from 12 to 24 to 48 hours, another hallmark of apoptosis, consistent with the higher levels of caspase activity at this timepoint. PCI-34051 does not stimulate Bid cleavage, a characteristic effect of the extrinsic apoptotic pathway. While P116 and J.RT3-T.5 are sensitive to PCI-34051, the PLCγ1-deficient J.gamma1 line reveals a marked decrease in the extent of PCI-34051-induced apoptosis. In addition, steady-state calcium levels strongly influence the apoptosis induced by PCI-34051. PCI-34051 induces cytochrome c release from mitochondria.


    Kinase Assay: For PCI-34051 characterization, measurements are perfomed in a reaction volume of 100 μL using 96-well assay plates in a fluorescence plate reader. For each isozyme. The HDAC protein in reaction buffer (50 mM HEPES, 100 mM KCl, 0.001% Tween-20, 5% dimethyl sulfoxide, pH7.4, supplemented with bovine serum albumin at concentrations of 0-0.05%) is mixed with PCI-34051 at various concentrations and allowed to incubate for 15 min. Trysin is added to a final concentration of 50 nM, and acetyl-gly-Ala-(N-acetyl-Lys)-amino-4-methylcoumarin is added to a final concentration of 25-100 μM to initiate the reaction. After a 30 min lag time, the fluorescence is measured over a 30 min time frame using an excitation wavelength of 335 nm and a detection wavelength of 460 nm. The increase in fluorescence wih time is used as the measure of the reaction rate.


    Cell Assay: Tumor cell lines and human umbilical vein endothelial cells are cultured for at least two doubling times, and growth is monitored at the end of PCI-34051 exposure using an Alamar Blue fluorometric cell proliferation assay as recommended by the manufacturer. PCI-34051 is assayed in triplicate wells in 96-well plates. The concentration required to inhibit cell growth by 50% (GI50) and 95% confidence intervals are estimated from nonlinear regression using a four-parameter logistic equation.

    In VivoAdministration of PCI-34051 and Dexamethasone reduces the eosinophilic inflammation and airway hyperresponsiveness in asthma to reduce the airway remodeling.
    Animal modelMice model of asthma
    Formulation & DosageA mouse model of asthma is utilized. Briefly, healthy female BALB/C mice (n=72) aged 6-8 weeks and weighing 18-22 g are used. Animals are housed independently in a pathogen-free room and provided ad libitum access to water and standard food. Animals are housed for 1 week prior to experiment onset. Mice are divided into six treatment groups: normal control, simple asthma, Dexamethasone, Tubastatin A HCl, PCI-34051, and Givinostat. Sensitization is carried out for mice in the last five groups on the 1st, 8th and 15th day using ovalbumin (OVA, 20 μg) and aluminum hydroxide gel (2 mg). 7 days after the last sensitization, OVA (20 mg/mL) atomization is performed using an ultrasonic atomizing device (3 mL/min for 30 min, 3 times/week for 8 weeks). Dexamethasone (2.0 mg/kg), TSA (0.5 mg/kg), PCI-34051 (0.5 mg/kg) and Givinostat (0.5 mg/kg) are administered via intraperitoneal injection 30 min before excitation. In the normal control group, normal saline is used instead of OVA.
    ReferencesLeukemia. 2008 May;22(5):1026-34; Inflamm Res. 2016 Dec;65(12):995-1008.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

     

    PCI-34051

    PCI-34051(5 muM) stimulates caspase-dependent apoptosis and induces caspase-3 activity in Jurkat cells treated for 2 days. Leukemia. 2008 May;22(5):1026-34. 
     

    PCI-34051

    PLCgamma1 activity is required for apoptosis induction by PCI-34051. Leukemia. 2008 May;22(5):1026-34. 
     

    PCI-34051

    PCI-34051-induced apoptosis is enhanced by Ca2+ effector thapsigargin and inhibited by the Ca2+ chelator BAPTA-AM. Leukemia.2008 May;22(5):1026-34. 


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