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    BG45
    BG45

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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 #: V0262
    CAS #: 926259-99-6Purity ≥98%

    Description: BG45 (BG-45) is a novel, potent and selective class I HDAC inhibitor with potential anticancer activity. It inhibits HDAC3, HDAC1, HDAC2, and HDAC6 with IC50s of 289 nM, 2.0 μM, 2.2 μM and >20 μM in cell-free assays, respectively. BG45 is relatively selective for inhibting HDAC3 (IC50 = 289 nM) over HDAC1, 2. It did not inihibit HDAC6 with IC50 >20 μM. BG45 signigicantly inhibited tumor growth in a mouse model of multiple myeloma either alone and synergistically in combination with bortezomib. HDAC3 represents a promising therapeutic target, and validate a prototype novel HDAC3 inhibitor BG45 in MM.

    ReferencesLeukemia. 2014 Mar;28(3):680-9.

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    Molecular Weight (MW)214.22
    FormulaC11H10N4O
    CAS No.926259-99-6
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 42 mg/mL (196.1 mM)
    Water: <1 mg/mL
    Ethanol: 2 mg/mL warmed (9.3 mM)
    Other info

    Chemical Name: N-(2-Aminophenyl)pyrazine-2-carboxamide; BG45

    InChi Key: LMWPVSNHKACEKW-UHFFFAOYSA-N

    InChi Code: InChI=1S/C11H10N4O/c12-8-3-1-2-4-9(8)15-11(16)10-7-13-5-6-14-10/h1-7H,12H2,(H,15,16)

    SMILES Code: O=C(C1=NC=CN=C1)NC2=CC=CC=C2N

    SynonymsBG45; BG-45; BG 45


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    In Vitro

    In vitro activity: BG45 causes significant cell growth inhibition and induces caspase-dependent apoptosis in a series of MM cells. In RPMI8226 cells, BG45 synergistically enhances bortezomib-induced cytotoxicity.


    Cell Assay: The growth inhibitory effects of BG45 in MM cell lines are assessed by measuring 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrasodium bromide (MTT) dye absorbance. To measure proliferation of MM cells, the rate of DNA synthesis is measured by [3H]thymidine uptake. Cell lines: MM.1S, RPMI8226, U266, H929, MM.1 R, RPMI-LR5, OPM1, OPM2 and RPMI-DOX40 cells.

    In VivoIn mice bearing MM.1S xenograft of human MM, BG45 (50 mg/kg, i.p.) significantly inhibits MM tumor growth. When in combination with bortezomib, BG45 (50 mg/kg, i.p.) enhances bortezomib-induced cytotoxicity.
    Animal modelMice bearing MM.1S xenograft
    Formulation & DosageDissolved in 10% dimethylacetamide in 10% Kolliphor HS15 in PBS; 50 mg/kg, 5 days a week;  i.p. injection
    References

    Leukemia. 2014 Mar;28(3):680-9.


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

     

    BG45

    HDAC3 selective inhibitor triggers significant MM cell growth inhibition. Leukemia. 2014 Mar;28(3):680-9.
     

    BG45

    HDAC3 inhibition enhances bortezomib-induced cytotoxicity. Leukemia. 2014 Mar;28(3):680-9. 
     

    BG45

    BG45 inhibits human MM cell growth and enhances bortezomib-induced cytotoxicity in vivo. Leukemia.2014 Mar;28(3):680-9. 


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