2. Neuronal Signaling NF-κB Metabolic Enzyme/Protease Immunology/Inflammation
  3. Monoamine Oxidase Reactive Oxygen Species (ROS) NO Synthase Interleukin Related
  4. Multi-target kinase-IN-10

Multi-target kinase-IN-10 (Compound 6l) is an orally active, blood-brain barrier-permeable, selective, reversible, and competitive MAO-B inhibitor with an IC50 of 0.0053 μM. Multi-target kinase-IN-10 competes with substrates for binding to the active site of MAO-B, chelates Cu2+ ions, inhibits Cu2+-induced ROS production, and reduces the release of NO, TNF-α, and IL-1β. Multi-target kinase-IN-10 ameliorates Parkinson's disease.

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Multi-target kinase-IN-10

Multi-target kinase-IN-10 Chemical Structure

CAS No. : 3022330-81-7

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Multi-target kinase-IN-10 Related Antibodies

Top Publications Citing Use of Products

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MAO-A MAO-B

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nNOS iNOS eNOS

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

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Description

Multi-target kinase-IN-10 (Compound 6l) is an orally active, blood-brain barrier-permeable, selective, reversible, and competitive MAO-B inhibitor with an IC50 of 0.0053 μM. Multi-target kinase-IN-10 competes with substrates for binding to the active site of MAO-B, chelates Cu2+ ions, inhibits Cu2+-induced ROS production, and reduces the release of NO, TNF-α, and IL-1β. Multi-target kinase-IN-10 ameliorates Parkinson's disease[1].

IC50 & Target[1]

IL-1β

 

MAO-B

0.0053 μM (IC50)

In Vitro

Multi-target kinase-IN-10 potently and selectively inhibits MAO-B with an IC50 of 0.0053 μM and a selectivity index greater than 1904.7[1].
Multi-target kinase-IN-10 (0.5-10.0 μM) dose-dependently inhibits LPS-induced release of NO, TNF-α and IL-1β in BV-2 microglia[1].
Multi-target kinase-IN-10 (2.5-10.0 μM) dose-dependently inhibits LPS-induced ROS production in BV-2 microglia, with inhibition rates of 18.9% and 41.7% at concentrations of 2.5 μM and 10.0 μM, respectively[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Multi-target kinase-IN-10 Related Antibodies

ELISA Assay[1]

Cell Line: LPS-stimulated
BV-2 cells
Concentration: 0.5-10.0 μM
Incubation Time: Unclear
Result: Exhibited potent TNF-α suppression, with inhibition rates
of 35.0%, 56.4%, and 82.1% at 0.5, 2.5, 10.0 μM, respectively.
Exhibited IL-1β suppression, with inhibition rates
of 37.5%, 54.5%, and 75.2% at 0.5, 2.5, 10.0 μM, respectively.
Parmacokinetics
Species Dose Route Cmax Tmax (Plasma) T1/2 AUC0-t Tmax (Brain)
Mice[1] 37.5 mg/kg p.o. 1177.55 (plasma) ng/mL 1.0 (plasma) h 1.96 (plasma) h 3522.34 (plasma) μg/L·h 1.0 (brain) h
In Vivo

Multi-target kinase-IN-10 (compound 6l) (7.5-37.5 mg/kg; i.g.; daily) significantly promotes behavioral recovery, restores striatal dopamine levels, reduces oxidative stress, attenuates neuroinflammation, and protects dopaminergic neurons in MPTP (HY-W114750)-induced subacute Parkinson's disease mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 (10 per group, MPTP-induced subacute model)[1]
Dosage: 7.5 mg/kg; 15 mg/kg; 37.5 mg/kg
Administration: i.g.; daily
Result: Significantly reduced motor deficits across all behavioral tests on days 1, 3, 7, and 14 at 37.5 mg/kg compared to the model group.
Showed significant improvements in most behavioral measures by day 7 at 15 mg/kg compared to the model group.
Showed a decreasing trend in motor deficits by day 3 and significant improvements by day 7 at 7.5 mg/kg compared to the model group.
Increased striatal dopamine levels by 60.5% at 37.5 mg/kg compared to the model group.
Reduced striatal malondialdehyde (MDA) content by 53.6% at 37.5 mg/kg compared to the model group.
Inhibited striatal TNF-α release by 67.1% and IL-6 release by 72.7% at 37.5 mg/kg relative to the model group.
Moderately restored dopamine levels, inhibited TNF-α release by 48.9%, and IL-6 release by 62.1% at 15 mg/kg compared to the model group.
Showed moderate dopamine recovery, inhibited TNF-α release by 24.2%, and IL-6 release by 45.8% at 7.5 mg/kg compared to the model group.
Significantly increased tyrosine hydroxylase (TH)-positive cell count in the substantia nigra pars compacta and enhanced TH-immunoreactive fiber density in the striatum at 37.5 mg/kg compared to the model group.
Molecular Weight

296.30

Formula

C17H13FN2O2
CAS No.
SMILES

OC1=CC=CC=C1C2=NN=C(OCC3=CC=C(F)C=C3)C=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Multi-target kinase-IN-10 Related Classifications

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Multi-target kinase-IN-103022330-81-7Monoamine OxidaseReactive Oxygen Species (ROS)NO SynthaseInterleukin RelatedMAONitric oxide synthasesNOSILCu2+IL-1βBV-2 cellparkinson's diseaseMAO-BTNF-αNOblood-brain barrierMAO-AROSInhibitorinhibitorinhibit

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