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TB5

Catalog No. T3596   CAS 948841-07-4

TB5 is a potent, selective and reversible inhibitor of hMAO-B.

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TB5 Chemical Structure
TB5, CAS 948841-07-4
Pack Size Availability Price/USD Quantity
5 mg In stock $ 41.00
10 mg In stock $ 66.00
25 mg In stock $ 121.00
50 mg In stock $ 197.00
100 mg In stock $ 316.00
1 mL * 10 mM (in DMSO) In stock $ 45.00
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Purity: 99.82%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description TB5 is a potent, selective and reversible inhibitor of hMAO-B.
Targets&IC50 MAO-B (human):0.11±0.01 μM. (Ki)
In vitro TB5 and TB8 interacts with the catalytic site of hMAO-B and hMAO-A with a competitive mode of inhibition. TB5 exhibits the best inhibitory activity and higher selectivity toward hMAO-B, with Ki and SI values of 0.11±0.01 μM 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 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].
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].
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].
Molecular Weight 336.25
Formula C15H14BrNOS
CAS No. 948841-07-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 55 mg/mL (163.57 mM)

TargetMolReferences and Literature

1. Mathew B, et al. Synthesis, Biochemistry, and Computational Studies of Brominated Thienyl Chalcones: A New Class of Reversible MAO-B Inhibitors. ChemMedChem. 2016 Jun 6;11(11):1161-71.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Neurodegenerative Disease Compound Library Inhibitor Library Anti-Metabolism Disease Compound Library Mitochondria-Targeted Compound Library Reprogramming Compound Library Anti-Parkinson's Disease Compound Library Bioactive Compound Library Bioactive Compounds Library Max Antidepressant Compound Library Neuronal Signaling Compound Library

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Keywords

TB5 948841-07-4 Metabolism Neuroscience Monoamine Oxidase MAO TB 5 Inhibitor inhibit TB-5 inhibitor

 

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