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SelDeg51

Chemical Structure : SelDeg51

CAS No.:

SelDeg51 (Selective Degrader of FKBP51)

Catalog No.: PC-21336Not For Human Use, Lab Use Only.

SelDeg51 (Selective Degrader of FKBP51) is a potent, selective FKBP51 PROTAC with Kd of 18 nM, Emax=90%.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

SelDeg51 (Selective Degrader of FKBP51) is a potent, selective FKBP51 PROTAC with Kd of 18 nM, Emax=90%.
SelDeg51 increases the Dexamethasone-induced expression of the endogenous GR target genes GILZand FKBP5, reflecting the removal of FKBP51-mediated repression of GR signalling.

Physicochemical Properties

M.Wt 1343.62
Formula C72H91FN8O14S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(1R)-3-(3,4-dimethoxyphenyl)-1-(4-((1-(3-(2-(((2S,4R)-1-(2-(1-fluorocyclopropane-1-carboxamido)-3,3-dimethylbutanoyl)-4-hydroxypyrrolidine-2-carboxamido)methyl)-5-(4-methylthiazol-5-yl)phenoxy)propyl)-1H-1,2,3-triazol-4-yl)methoxy)phenyl)propyl (2S)-1-((S)-2-cyclohexyl-2-(3,4,5-trimethoxyphenyl)acetyl)piperidine-2-carboxylate

References

1. Thomas M Geiger, et al. Angew Chem Int Ed Engl. 2023 Nov 9:e202309706.

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