| Name | TB5 |
| Description | TB5 is a potent, selective, and reversible inhibitor of hMAO-B. |
| Cell Research | 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)[1]. |
| 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[1]. |
| In vitro | TB5 and TB8 interact competitively with the catalytic sites of hMAO-B and hMAO-A. TB5 shows the highest inhibitory activity and selectivity toward hMAO-B, with Ki and SI values of 0.11±0.01 μM and 13.18, respectively. Inhibition by TB5 (hMAO-B) and TB8 (hMAO-A) is fully reversible after 24 hours of dialysis. Cytotoxicity studies reveal TB5 is non-toxic at 5 and 25 μM, with cell viabilities of 95.75% and 84.59%, respectively [1]. |
| In vivo | Compounds are initially dissolved in DMSO (5 mg/mL), then further diluted with a PBS/EtOH mixture (70:30). To elucidate the critical interactions dictating selectivity and potency, kinetic analyses of TB5 and TB8 are conducted. Lineweaver–Burk plots, a total of five, are created to compare the catalytic rates of MAO-B and MAO-A at various substrate concentrations (0.1-1 μM) in both the absence and presence of TB5 and TB8 at differing concentrations. The initial plot reveals the baseline enzyme activity without inhibitors, while the subsequent four plots show the impact of varying concentrations of TB5 and TB8[1]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 55 mg/mL (163.57 mM)
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| Keywords | MAO | Monoamine Oxidase | TB5 | TB 5 | Inhibitor | inhibit | TB-5 |
| Inhibitors Related | Hydroxyamine hydrochloride | Harmine | Hydralazine hydrochloride | Safinamide | Azure B | 1,4-Naphthoquinone | Paeonol | Isatin | Methylene Blue | Methylene Blue trihydrate | Furazolidone | Allylthiourea |
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United States
