SP3N
SP3N is a specific degrader of the prolyl isomerase FKBP12. As a prodrug, SP3N is metabolized by Diamine oxidase into the active aldehyde metabolite SP3CHO (HY-161795). SP3N induces the proximity of FKBP12 to the SCFFBXO22 E3 ligase complex, thereby triggering the polyubiquitination and proteasomal degradation of FKBP12. SP3N can be used in cancer research.
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- Fòrmula: C39H57N3O10
- Peso molecular:727.88
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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
IC50 & Target
[1]|
FKBP12 |
In Vitro
SP3N (1 nM-10 μM; 1-16 h) potently degrades FKBP12 in KBM7 iCas9 FKBP12-BFP-P2A-mCherry reporter cells in a time- and dose-dependent manner, and this degradation depends on the ubiquitin-proteasome system and Cullin-RING ligase activity[1].
SP3N (1 μM; 16 h) degrades FKBP12 in HEK293T cells, with no detectable off-target degradation across the proteome after 16 h of 1 μM treatment[1].
SP3N (0.001-20 μM; 16 h) dose-dependently reduces FKBP12 protein levels in HEK293T Nluc-3xFlag-FKBP12-NLS cells after 16 h of treatment[1].
SP3N requires metabolic conversion by amine oxidases (such as DAO) to an active species to induce FKBP12 degradation in KBM7 iCas9 FKBP12-BFP-P2A-mCherry reporter cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293T Nluc-3xFlag-FKBP12-NLS cells
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Concentration:0.001 μM, 0.01 μM, 0.1 μM, 1 μM, 10 μM, 20 μM
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Incubation Time:16 h
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Result:Reduced FKBP12 protein levels in a dose-dependent manner.
Started detectable degradation at 0.01 μM.
Achieved near-complete degradation at 20 μM.
Chemical Information
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Peso molecular 727.88
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Fòrmula C39H57N3O10
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SMILES
COC1=CC=C(CC[C@@H](OC([C@@H]2CCCCN2C(C(C(C)(C)CC)=O)=O)=O)C3=CC(NC(CCOCCOCCOCCN)=O)=CC=C3)C=C1OC
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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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
SP3N Related Classifications
HY-161794 Related Classifications
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