Epibestatin
Epibestatin is an epimer of Bestatin (HY-B0134), a DPP4 inhibitor and protease inhibitor, with an IC50 of 17 μM against DPP4. As a stabilizer, Epibestatin binds to the cleft between 14-3-3 protein and plant proton pump PMA2, selectively stabilizing their interaction without affecting other 14-3-3 client proteins. Epibestatin triggers stomatal opening in leaf epidermis of Commelina communis. Epibestatin can be used in studies related to type 2 diabetes.
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- CAS. Nr.: 61046-23-9
- Formel: C16H24N2O4
- Molecular Weight:308.37
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
DPP-4 17 μM (IC50) |
In Vitro
Epibestatin (50 μM) stabilizes the interaction between purified 14-3-3 protein and PMA2-CT52 with a KD of 1.8 μM, as measured via surface plasmon resonance[3].
Epibestatin (50 μM; 3 h) induces stomatal opening in isolated Commelina communis leaf epidermis to an average width of 3.2 μm after 3 hours of incubation[3].
Epibestatin does not stabilize the interaction between purified 14-3-3 protein and any of the tested alternative targets (Raf1, p53, Cdc25C, RNF11, Mlf1, AICD, Cby, YAP), demonstrating selectivity for the 14-3-3/PMA2 complex[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 61046-23-9
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Molecular Weight 308.37
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Formel C16H24N2O4
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SMILES
CC(C[C@H](NC([C@H](O)[C@H](N)CC1=CC=CC=C1)=O)C(O)=O)C
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[1]. Kawaguchi M, et al. A time-resolved fluorescence probe for dipeptidyl peptidase 4 and its application in inhibitor screening. Chemistry (Weinheim an der Bergstrasse, Germany). 2010 Dec 03;16(45):13479-86. [Content Brief]
[3]. Rose R, et al. Identification and structure of small-molecule stabilizers of 14-3-3 protein-protein interactions. Angew Chem Int Ed Engl. 2010 Jun 1;49(24):4129-32. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Epibestatin Related Classifications
HY-W723158A Related Classifications
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