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    Droxinostat (NS41080)
    Droxinostat (NS41080)

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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 #: V0290
    CAS #: 99873-43-5Purity ≥98%

    Description: Droxinostat (formerly NS-41080) is a novel, potent, selective inhibitor of histone deacetylase (HDAC) with potential anticancer activity. It inhibits HDAC6 and HDAC8 with IC50s of 2.47 μM and 1.46 μM, and shows >8-fold selectivity overHDAC3.

    References: Cancer Res. 2006 Feb 15;66(4):2367-75; Mol Cancer Ther. 2010 Jan;9(1):246-56.

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    Molecular Weight (MW)243.69
    FormulaC11H14ClNO3
    CAS No.99873-43-5
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 49 mg/mL (201.1 mM)
    Water: <1 mg/mL
    Ethanol: 49 mg/mL (201.1 mM)
    Solubility (In vivo)30% propylene glycol, 5% Tween 80, 65% D5W: 30 mg/mL
    Synonyms

    Synonym: NS 41080; NS41080; NS-41080; 4(4Chloro2methylphenoxy)Nhydroxybutanamide

    Chemical Name: 4-(4-chloro-2-methylphenoxy)-N-hydroxybutanamide

    InChi Key: JHSXDAWGLCZYSM-UHFFFAOYSA-N

    InChi Code: InChI=1S/C11H14ClNO3/c1-8-7-9(12)4-5-10(8)16-6-2-3-11(14)13-15/h4-5,7,15H,2-3,6H2,1H3,(H,13,14)

    SMILES Code: O=C(NO)CCCOC1=CC=C(Cl)C=C1C


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    In Vitro

    In vitro activity: Droxinostat is originally identified as a sensitizer of PPC-1 cells to FAS and TRAIL by downregulating the expression of c-Fas-associated death domain-like interleukin-1-converting enzyme-like inhibitory protein (c-FLIP). In PPC-1 cells cultured in suspension but not adherent conditions, Droxinostat (20 μM–60 μM) sensitizes cells to anoikis by initially activating caspase 8 with subsequent activation of the mitochondrial pathway. Similarly, Droxinostat also sensitizes other cancer cell lines including PC-3, DU-145, T47D, and OVCAR-3, but not LNCaP or MB-MDA-468, to anoikis or CH-11-induced apoptosis. However, the direct targets of Droxinostat remains enigma until recently. It is revealed that in histone deacetylases (HDAC) isoform 1-10, Droxinostat selective inhibits HDAC3, 6, and 8, with IC50 values of 16.9 μM, 2.47 μM, and 1.46 μM, respectively, without inhibiting other HDAC members (IC50 > 20 μM). In MCF-7 breast cancer cells, Droxinostat (10 μM–100 μM) sensitizes cells to apoptosis by decreasing c-FLIPL and c-FLIPS expression, reducing cell survival, and inducing apoptosis


    Kinase Assay: HDAC inhibition is assessed using the CycLex HDACs fluorometric assay according to the manufacturer's protocol and using crude nuclear extract from HeLa cells (principally HDAC1 and HDAC2). The relative activity is expressed as (fluorescence intensity of treated samples/fluorescence intensity of controls) × 100


    Cell Assay: PPC-1 cells (1 × 104) are seeded overnight into 96-well flat-bottomed plates in 100 μL of medium containing 2.5% FCS. The next day, Droxinostat is added. CH-11 antibody (100 ng/mL) is then added and the cells are incubated for 24 hours before assessing cell viability by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) dye reduction assay.

    In VivoIn SCID mice models, Droxinostat (30 μM)-treated PPC-1 cells results in decreased distant tumor formation than untreated cells.
    Animal modelMice
    Formulation & Dosage30 μM
    References

    Cancer Res. 2006 Feb 15;66(4):2367-75; J Natl Cancer Inst. 2007 May 16;99(10):811-22; Mol Cancer Ther. 2010 Jan;9(1):246-56.


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

     
    Droxinostat
    Droxinostat inhibits HDAC activity. Mol Cancer Ther. 2010 Jan;9(1):246-56.
     
    Droxinostat
    HDACis sensitize resistant cells to FAS. Mol Cancer Ther. 2010 Jan;9(1):246-56.
     
    Droxinostat
    Genetic knockdown of HDAC3, HDAC6, and HDAC8 and sensitization to death receptor ligands. Mol Cancer Ther. 2010 Jan;9(1):246-56.


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