JLK-6
JLK-6 is a rhomboid protease GlpG inhibitor. JLK-6 reduces the production of Amyloid β-peptide by altering the cleavage of β-amyloid precursor protein by γ-secretase, with no effect on the cleavage of Notch receptors. JLK-6 can be used in research related to Alzheimer's disease.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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: 62252-26-0
- 分子式: C10H8ClNO3
- 分子量:225.63
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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
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
製品説明
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
30 μM
Compound: 24; JLK6
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Inhibition of gamma secretase mediated amyloid beta level reduction in HEK293 cells expressing APP after 72 hrs by chemiluminescence assay
Inhibition of gamma secretase mediated amyloid beta level reduction in HEK293 cells expressing APP after 72 hrs by chemiluminescence assay
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[PMID: 27045975] |
体外実験
JLK-6 (3-60 μM; 7 h) potently reduces Aβ production in bAPPswe-overexpressing HEK293 cells with an IC50 of 30-60 μM, while sparing Notch signaling and other protease pathways without inducing cell toxicity at 100 μM[1].
JLK-6 (10 μM; 1 h) irreversibly inhibits E. coli GlpG rhomboid protease, as no enzyme activity recovery is observed after dilution of the inhibitor-enzyme complex[2].
JLK-6 forms a double-bonded end product with E. coli GlpG rhomboid protease, resulting in a detectable mobility shift on SDS-PAGE[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293 cells stably overexpressing Swedish mutant β-amyloid precursor protein (bAPPswe)
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Concentration:3 μM, 10 μM, 30 μM, 60 μM
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Incubation Time:7 h
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Result:Reduced Aβ production in a concentration-dependent manner: 3 μM and 10 μM caused partial reduction, 30 μM caused further reduction, and 60 μM resulted in near-complete inhibition of Aβ production.
Exhibited an IC50 of approximately 30-60 μM in this assay.
Did not interfere with the processing of Notch receptor, cadherins, CD44, α-secretase, β-secretase, or GSK3β kinase.
Showed no cell toxicity at 100 μM.
化学情報
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CAS 番号 62252-26-0
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分子量 225.63
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分子式 C10H8ClNO3
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SMILES
O=C1C2=CC(N)=CC=C2C(Cl)=C(OC)O1
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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]. Peuchmaur M, et al. Further characterization of a putative serine protease contributing to the γ-secretase cleavage of β-amyloid precursor protein. Bioorganic & medicinal chemistry. 2013 Feb 15;21(4):1018-29. [Content Brief]
[2]. Goel P, et al. Discovery and Biological Evaluation of Potent and Selective N-Methylene Saccharin-Derived Inhibitors for Rhomboid Intramembrane Proteases. Biochemistry. 2017 Dec 26;56(51):6713-6725. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
JLK-6 関連分類
HY-103538 関連分類
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