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    HPOB
    HPOB

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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 #: V0265
    CAS #: 1429651-50-2Purity ≥98%

    Description: HPOB is a novel, potent and selective inhibitor of histone deacetylase 6 (HDAC6) inhibitor with potential anticancer activity. It inhibits HDAC6 with an IC50 of 56 nM, and shows >30-fold selectivity for HDAC6 over other HDAC isoforms. 

    ReferencesProc Natl Acad Sci U S A. 2013 Sep 24;110(39):15704-9. 

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    Molecular Weight (MW)314.34
    FormulaC17H18N2O4
    CAS No.1429651-50-2
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 62 mg/mL (197.2 mM) 
    Water: <1 mg/mL
    Ethanol: 38 mg/mL warmed (120.9mM)
    Other infoSMILES: OCCN(C(CC1=CC=C(C(NO)=O)C=C1)=O)C2=CC=CC=C2
    InChI Code: InChI=1S/C17H18N2O4/c20-11-10-19(15-4-2-1-3-5-15)16(21)12-13-6-8-14(9-7-13)17(22)18-23/h1-9,20,23H,10-12H2,(H,18,22)
    InChI Key: RFAZNTABYJYOAR-UHFFFAOYSA-N
    SynonymsHPOB; 4-[(hydroxyamino)carbonyl]-N-(2-hydroxyethyl)-N-phenyl-benzeneacetamide


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    In Vitro

    In vitro activity: In normal (HFS) and transformed (LNCaP, A549, and U87) cells, HPOB induces acetylation of α-tubulin, however, not histones, and inhibits cell growth, however, not viability. In HFS cells, HPOB enhances transformed cell death induced by etoposide, doxorubicin, or SAHA. HPOB also enhancing etoposide-induced transformed cell death via the apoptotic pathway in transformed cells.


    Kinase Assay: In vitro activities of the 11 recombinant human zinc-dependent HDAC enzymes are detected by fluorigenic release of 7-amino-4-methylcoumarin from substrate upon deacetylase enzymatic activity. A series of dilutions of the unique HDAC6 compound, tubacin, and SAHA are prepared with 10% DMSO in HDAC assay buffer, and 5 μL of the dilution was added to a 50-μL reaction so that the final concentration of DMSO is 1% in all of the reactions. The enzymatic reactions are conducted in duplicate at 37 °C for 30 min in a 50-μL mixture containing HDAC assay buffer, 5 μg BSA, an HDAC substrate, an HDAC enzyme, and a test compound. After enzymatic reactions, 50 μL of 2× HDAC developer is added to each well, and the plate is incubated at room temperature for an additional 15 min. Fluorescence intensity is measured at an excitation of 360 nm and an emission of 460 nm using a Synergy microplate reader. Negative (no enzyme, no inhibitor, a drug with no HDAC inhibition activity) and positive controls (known HDAC inhibitor SAHA) are included in the assays. IC50 is determined at the drug concentration that results in 50% reduction of HDAC activity compared with the control. 


    Cell Assay: Normal (HFS) and transformed (LNCaP, A549, and U87) cells are cultured with indicated doses of HPOB for 72 h. Five micromolars SAHA is a positive control.Graphs were constructed using Prism 5. 

    In VivoIn mice bearing CWR22 human prostate cancer xenografts, HPOB (300 mg/kg/d i.p.), when in combination with SAHA, causes suppression of the growth of established tumors, while produces no significant suppression when used alone.
    Animal modelMice bearing CWR22 human prostate cancer xenografts
    Formulation & DosageDissolved in DMSO; 300 mg/kg daily; i.p. injection.
    References

    Proc Natl Acad Sci U S A. 2013 Sep 24;110(39):15704-9.


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

     

    HPOB

    Effects of HPOB on cell growth and viability and acetylated patterns of proteins and histones in normal and transformed cells in culture. Proc Natl Acad Sci U S A. 2013 Sep 24;110(39):15704-9. 
     

    HPOB

    HPOB enhances etoposide-, doxorubicin-, and SAHA-induced transformed cell death but not normal cell death. Proc Natl Acad Sci U S A. 2013 Sep 24;110(39):15704-9. 
     

    HPOB

    HPOB enhances anticancer effects of SAHA in mice bearing human prostate cancer CWR22 xenograft. Proc Natl Acad Sci U S A. 2013 Sep 24;110(39):15704-9. 


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