FX 2149
FX 2149 is a blood-brain barrier-permeable LRRK2 inhibitor. FX 2149 inhibits the GTP-binding activity of LRRK2, reduces the kinase activity of LRRK2, and attenuates LPS (HY-D1056)-induced upregulation of LRRK2. FX 2149 alleviates mutant LRRK2-induced neurodegeneration, microglial activation, static aggregation of mitochondria and lysosomes, reduces apoptosis, and improves mitochondrial and lysosomal motility deficits in neurites. FX 2149 can be used in research related to Parkinson's disease.
For research use only. We do not sell to patients.
- CAS No.: 1842427-90-0
- Formula: C15H17N3O3S
- Molecular Weight:319.38
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
In Vitro
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human neuroblastoma SH-SY5Y cells expressing G2019S-LRRK2
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Concentration:50 nM, 100 nM, 200 nM
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Incubation Time:48 h
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Result:Increased the viability of G2019S-LRRK2-expressing cells compared to vehicle-treated cells.
Reduced the percentage of TUNEL-positive G2019S-LRRK2-expressing cells to levels.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:G2019S-LRRK2-BAC transgenic (6-12 weeks of age)[1]
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Dosage:10 mg/kg
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Administration:i.p.; single dose
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Result:Reduced brain LRRK2 GTP binding activity to levels.
Significantly reduced brain LRRK2 kinase activity.
Reduced 4E-BP phosphorylation to 15% of the untreated transgenic control group.
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Animal Model:G2019S-LRRK2-BAC transgenic (6-12 weeks of age)[1]
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Dosage:10 mg/kg
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Administration:i.p.; single pre-LPS dose followed by twice daily doses; 3 days
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Result:Significantly reduced LPS-induced LRRK2 expression and phosphorylated-LRRK2 immunoactivity in the substantia nigra.
Reduced LPS-induced isolectin B4 positive immunostaining to ~43% of the LPS-alone treated group, representing a 57% reduction in microglia activation.
Left dopaminergic neuron marker (TH) immunostaining unchanged across groups.
- Kinase activity and phosphorylation assays
- Neurotoxicity Study
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Annexin V plus membrane-impermeant dye apoptosis staining
- Human pluripotent stem cell midbrain dopaminergic neuron differentiation
- Apoptosis Solutions
- Protocol for Kinase activity and phosphorylation assays
- Lysosome and acidic-vesicle live-cell staining
Chemical Information
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CAS No. 1842427-90-0
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Molecular Weight 319.38
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Formula C15H17N3O3S
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SMILES
O=C(NCCC)C=1C=CC=C(C1)NS(=O)(=O)C=2C=NC=CC2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Li T, et al. A novel GTP-binding inhibitor, FX2149, attenuates LRRK2 toxicity in Parkinson's disease models. PloS one. 2015;10(3):e0122461. [Content Brief]
[2]. Thomas JM, et al. 68 and FX2149 Attenuate Mutant LRRK2-R1441C-Induced Neural Transport Impairment. Frontiers in aging neuroscience. 2016;8:337. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
FX 2149 Related Classifications
HY-169900 Related Classifications
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