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 番号: 1427947-55-4
- 分子式: C21H21N3O2
- 分子量:347.41
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
体外実験
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.
化学情報
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CAS 番号 1427947-55-4
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分子量 347.41
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)