(R)-SM875
(R)-SM875 is a cellular prion protein (PrP) degrader with an IC50 of 3 μM in HEK293 cells. (R)-SM875 interacts with PrP folding intermediates, binds to a binding pocket unique to FI-PrP, inhibits PrPC maturation, blocks prion replication, and induces cytotoxicity, autophagy, PrPC aggregation, as well as lysosome-dependent autophagy-mediated post-translational degradation of PrPC, without altering the mRNA level of PrPC. (R)-SM875 can be used in research related to prion diseases.
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- CAS. Nr.: 2715974-36-8
- Formel: C19H16BrN3O3
- Molecular Weight:414.25
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Speicherung:
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
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Biologische Aktivität
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Biologische Aktivität
Beschreibung
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PrP 3 μM (IC50) |
In Vitro
(R)-SM875 interacts with the ADMPC chiral stationary phase model with a more favorable Gibbs free energy (-7.5 kcal/mol) and a broader range of binding interactions compared to its (S)-enantiomer[1].
(R)-SM875 (0.1-30 μM; 48 h) potently reduces cellular prion protein levels in HEK293 cells with an IC50 of 3 μM[1].
(R)-SM875 (0.1-30 μM; 48 h) exhibits cytotoxicity in HEK293 cells within its active concentration range, with an LD50 above 30 μM in ZR-75-1 cells and above 10 μM in RK-13 cells[1].
(R)-SM875 (500 ns) forms dynamic, stable interactions with the prion protein folding intermediate over a 500 ns molecular dynamics simulation, including π-π stacking, π-cation, and hydrogen bond interactions with key PrP residues[1].
(R)-SM875 dose-dependently lowers mouse PrPC levels in stably transfected HEK293 cells[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
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Concentration:0.1-30 μM
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Incubation Time:48 h
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Result:Reduced cellular prion protein levels in a dose-dependent manner, with an IC50 of 3 μM.
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Cell Line:HEK293, ZR-75-1, and RK-13 cells
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Concentration:0.1-30 μM
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Incubation Time:48 h
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Result:Caused cytotoxicity in HEK293 cells within its active concentration range.
Showed an LD50 higher than 30 μM in ZR-75-1 cells.
Showed an LD50 higher than 10 μM in RK-13 cells.
Chemical Information
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CAS. Nr. 2715974-36-8
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Molecular Weight 414.25
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Formel C19H16BrN3O3
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SMILES
O=C1NC2=C(C=NN2C3=CC=C(C=C3)Br)[C@@H](C4=CC(OC)=C(C=C4)O)C1
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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
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Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
(R)-SM875 Related Classifications
HY-150286A Related Classifications
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