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.
For research use only. We do not sell to patients.
- Formula: C39H57N3O10
- Molecular Weight:727.88
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Storage:
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
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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FKBP12 |
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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Molecular Weight 727.88
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
SP3N Related Classifications
HY-161794 Related Classifications
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