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.
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- CAS No.: 62252-26-0
- Formule: C10H8ClNO3
- Masse moléculaire:225.63
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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Cell Line
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Type | Value | Description | References |
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| 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] |
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.
Chemical Information
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CAS No. 62252-26-0
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Masse moléculaire 225.63
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Formule C10H8ClNO3
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SMILES
O=C1C2=CC(N)=CC=C2C(Cl)=C(OC)O1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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