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    TB5
    TB5

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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 #: V0089
    CAS #: 948841-07-4 Purity ≥98%

    Description: TB5 is a novel, potent, selective, reversible and competitive inhibitor of hMAO-B (human monoamine oxidase-B) with Ki value of 0.11±0.01 μM. TB5 is can be potentially used for the treatment of neurodegenerative disorders like PD and AD (Parkinson's and Alzheimer's diseases). In addition, TB5 was found to be nontoxic at 5 and 25 μm, with 95.75% and 84.59 % viability among cells, respectively. 

    References:  2016 Jun 6;11(11):1161-71. 

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    Molecular Weight (MW) 336.25
    Formula C15H14BrNOS
    CAS No. 948841-07-4 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 10mM
    Water: N/A
    Ethanol: N/A
    Chemical Name (2E)-1-(5-bromothiophen-2-yl)-3-[4-(dimethylamino)phenyl]prop-2-en-1-one
    Synonyms TB5, TB 5, TB-5
    SMILES Code O=C(C1=CC=C(Br)S1)/C=C/C2=CC=C(N(C)C)C=C2


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    In Vitro

    In vitro activity: TB5 interacts with the catalytic site of hMAO-B and hMAO-A with a competitive mode of inhibition. TB5 shows the best inhibitory activity and higher selectivity toward hMAO-B, with Ki and SI values of 0.11±0.01μM and 13.18, respectively. hMAO-B inhibition by compound TB5 and hMAO-A inhibition by compound TB8 are completely reversed after 24 h of dialysis. Cytotoxicity studies show TB5 is nontoxic at 5 and 25 μM, resulting in cell viabilities of 95.75% and 84.59 %, respectively. 


    Kinase Assay: Compounds are dissolved in DMSO (5 mg/mL) and diluted with PBS/EtOH (70:30).Kinetic analyses are carried out for TB5 and TB8. A set of Lineweaver–Burk plots are constructed in the absence and presence of various concentrations of compounds TB5 and TC8. The set consists of five graphs, each constructed by measuring MAO-B and MAO-A catalytic rates at different substrate concentrations (0.1-1 μM). The first Lineweaver–Burk plot is constructed in the absence of inhibitor, while the remaining four graphs are constructed in the presence of different concentrations of TB5 and TB8


    Cell Assay: In vitro cytotoxicity of brominated thiophene chalcones and standard MAO inhibitors are tested in human HepG2 hepatic cancer cells at three different concentrations (1, 5 and 25 μM).

    In VivoTest compounds are dissolved in DMSO (5 mg/mL) and diluted with PBS/EtOH (70:30).Kinetic analyses are carried out for TB5 and TB8. A set of Lineweaver–Burk plots are constructed in the absence and presence of various concentrations of compounds TB5 and TC8. The set consists of five graphs, each constructed by measuring MAO-B and MAO-A catalytic rates at different substrate concentrations (0.1-1 μM). The first Lineweaver–Burk plot is constructed in the absence of inhibitor, while the remaining four graphs are constructed in the presence of different concentrations of TB5 and TB8
    Animal model
    Formulation & Dosage 5 mg/mL
    References  2016 Jun 6;11(11):1161-71. 


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

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