LRRK2-IN-22
LRRK2-IN-22 is a LRRK2 inhibitor, with IC50 values of 315.7 nM and 255.4 nM against LRRK2WT and LRRK2G2019S, respectively. LRRK2-IN-22 effectively inhibits LRRK2 kinase activity and downstream Rab10 phosphorylation, reduces ROS, and exhibits low cytotoxicity. LRRK2-IN-22 can be used for research on Parkinson's disease.
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- CAS. Nr.: 1427947-55-4
- Formel: C21H21N3O2
- Molecular Weight:347.41
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biologische Aktivität
Beschreibung
In Vitro
LRRK2-IN-22 (Compound C-298) (0-10 μM; 24 h) exhibits low cytotoxicity in untransfected HEK293T cells, with an IC50 of 3273 nM after 24 h of treatment[1].
LRRK2-IN-22 (1-10 μM; 24 h) potently and dose-dependently inhibits ROS production, and its effect is stronger in HEK293T cells overexpressing LRRK2G2019S than in cells overexpressing wild-type (WT) LRRK2[1].
LRRK2-IN-22 (30-10000 nM; 4 h) potently and dose-dependently inhibits the phosphorylation of LRRK2 (Ser935) and Rab10 (Thr73), and exhibits higher potency against the LRRK2G2019S mutant than wild-type LRRK2 in HEK293T cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293T cells overexpressing WT or G2019S mutant LRRK2
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Concentration:30, 100, 300, 1000, 3000 and 10000 nM
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Incubation Time:4 h
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Result:Suppressed phosphorylation of LRRK2 at Ser935 and Rab10 at Thr73 in a dose-dependent manner.
Inhibited pSer935-LRRK2 with an IC50 of 341.4 nM in WT LRRK2-overexpressing cells and 226.7 nM in G2019S LRRK2-overexpressing cells.
Inhibited pThr73-Rab10 with an IC50 of 425.7 nM in WT LRRK2-overexpressing cells and 231.2 nM in G2019S LRRK2-overexpressing cells.
- Kinase activity and phosphorylation assays
- Western Blot
- Cell Cytotoxicity Assay
- Mammalian live/dead viability and cytotoxicity staining
- ROS/oxidative-stress fluorescent staining
- Human pluripotent stem cell midbrain dopaminergic neuron differentiation
- Protocol for Kinase activity and phosphorylation assays
- Cell Viability Determination by MTT Colorimetric Assay
Chemical Information
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CAS. Nr. 1427947-55-4
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Molecular Weight 347.41
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Formel C21H21N3O2
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SMILES
COC1=CC=C(CC(N2CC=C(C3=CNC4=C3C=CC=N4)CC2)=O)C=C1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)