Lu AF58786
Lu AF58786 is a potent and selective LRRK2 inhibitor with an IC50 of 12 nM. Lu AF58786 also exhibits inhibition activity against LRRK2 G2019S and LRRK2 A2016T with IC50s of 19 and 93 nM. Lu AF58786 inhibits phosphorylation of LRRK2, Rab10 and Rab12 in human peripheral blood mononuclear cells. Lu AF58786 can be used for parkinson’s disease research.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1632368-13-8
- 分子式: C19H16N6
- 分子量:328.37
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
IC50 & Target
[1]|
LRRK2 G2019S 19 nM (IC50) |
LRRK2 A2016T 93 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
17 nM
Compound: 23
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Inhibition of human wild type LRRK2 phosphorylation at ser935 expressed in BacMam transduced HEK293 cells after 48 hrs by in-cell Western assay
Inhibition of human wild type LRRK2 phosphorylation at ser935 expressed in BacMam transduced HEK293 cells after 48 hrs by in-cell Western assay
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[PMID: 29023112] |
化学情報
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CAS 番号 1632368-13-8
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分子量 328.37
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分子式 C19H16N6
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SMILES
N#CC1=CNC2=NC(NC3=NN(C)C=C3)=CC(C4=CC(C)=CC=C4)=C12
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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
[1]. Thirstrup K, et al. Selective LRRK2 kinase inhibition reduces phosphorylation of endogenous Rab10 and Rab12 in human peripheral mononuclear blood cells. Sci Rep. 2017 Aug 31;7(1):10300. [Content Brief]
[2]. Williamson DS, et al. Design of Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitors Using a Crystallographic Surrogate Derived from Checkpoint Kinase 1 (CHK1). J Med Chem. 2017 Nov 9;60(21):8945-8962. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Lu AF58786 関連分類
HY-180320 関連分類
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