GSI-136
GSI-136 is an inhibitor of γ-secretase with an IC50 of 3 nM. GSI-136 can lead to a dose-dependent reduction of Aβ40 levels in diethylamine-extracted brain homogenates of C57BL/6 mice. GSI-136 can be studied in medicinal chemistry and Alzheimer's disease research.
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- No. CAS: 443989-01-3
- Fòrmula: C11H18ClNO3S2
- Peso molecular:311.85
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
29 nM
Compound: 1
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Inhibition of gamma-secretase-mediated cleavage of human APP expressed in CHO cells assessed as reduction in amyloid beta40 production after 24 hrs by double sandwich ELISA
Inhibition of gamma-secretase-mediated cleavage of human APP expressed in CHO cells assessed as reduction in amyloid beta40 production after 24 hrs by double sandwich ELISA
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[PMID: 19443228] |
| CHO | EC50 |
29 nM
Compound: 1
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Inhibition of gamma-secretase-mediated cleavage of human APP expressed in CHO cells assessed as reduction in amyloid beta42 production after 24 hrs by double sandwich ELISA
Inhibition of gamma-secretase-mediated cleavage of human APP expressed in CHO cells assessed as reduction in amyloid beta42 production after 24 hrs by double sandwich ELISA
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[PMID: 19443228] |
| CHO | IC50 |
25 nM
Compound: 9
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Inhibition of gamma-secretase expressed in CHO cells expressing human recombinant APP assessed as amyloid beta40 aggregation
Inhibition of gamma-secretase expressed in CHO cells expressing human recombinant APP assessed as amyloid beta40 aggregation
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[PMID: 19012391] |
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 443989-01-3
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Peso molecular 311.85
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Fòrmula C11H18ClNO3S2
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SMILES
O=S(C1=CC=C(S1)Cl)(N[C@H](CO)C(CC)CC)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[1]. Chinthakindi, P. K., et al., (2017). Sulfonimidamides in Medicinal and Agricultural Chemistry. Angewandte Chemie (International ed. in English), 56(15), 4100-4109. [Content Brief]
[2]. Sehgelmeble, F., et al., (2012). Sulfonimidamides as sulfonamides bioisosteres: rational evaluation through synthetic, in vitro, and in vivo studies with γ-secretase inhibitors. ChemMedChem, 7(3), 396-399. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
GSI-136 Related Classifications
HY-117236 Related Classifications
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