SelDeg51
SelDeg51 is a selective FKBP51 PROTAC degrader with a Kd value of 18 nM and a Dmax of 90%. SelDeg51 induces proteasomal degradation of FKBP51 via the FKBP51:SelDeg51:VCB ternary complex and reactivates the glucocorticoid receptor signaling pathway. SelDeg51 can be used for research on stress-related mental disorders, chronic pain, and obesity.
(Pink: Target protein ligand; Blue: VHL ligand (HY-125905); Black: linker).
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- No. CAS: 3036372-80-9
- Fòrmula: C72H91FN8O14S
- Peso molecular:1343.60
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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]|
VHL |
FKBP51 18 nM (Kd) |
In Vitro
SelDeg51 (0.6-10 μM; 0-48 h) degrades FKBP51 in a time-dependent and reversible manner in HEK293T cells, with high selectivity for FKBP12[1].
SelDeg51 (250 nM) enhances Dexamethasone (HY-14648)-induced expression of endogenous glucocorticoid receptor target genes GILZ and FKBP5 in A549 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 cells
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Concentration:1 μM
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Incubation Time:0, 2, 4, 6, 8, 24 and 48 h
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Result:Reduced FKBP51 protein levels.
Did not affact FKBP12 protein levels.
Chemical Information
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No. CAS 3036372-80-9
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Peso molecular 1343.60
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Fòrmula C72H91FN8O14S
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SMILES
O=C(N1CCCC[C@H]1C(O[C@H](CCC2=CC(OC)=C(OC)C=C2)C3=CC=C(OCC4=CN(CCCOC5=C(CNC([C@@H]6C[C@@H](O)CN6C([C@H](C(C)(C)C)NC(C7(CC7)F)=O)=O)=O)C=CC(C8=C(C)N=CS8)=C5)N=N4)C=C3)=O)[C@H](C9=CC(OC)=C(OC)C(OC)=C9)C%10CCCCC%10
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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)
SelDeg51 Related Classifications
HY-181289 Related Classifications
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