14-3-3σ/ERα stabilizer 181

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Chemical Structure : 14-3-3σ/ERα stabilizer 181

Catalog No.: PC-21138Not For Human Use, Lab Use Only.

14-3-3σ/ERα stabilizer 181 is a selective and highly potent covalent stabilizer of 14-3-3σ/ERα PPI complex with EC50 of 1 uM.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

14-3-3σ/ERα stabilizer 181 is a selective and highly potent covalent stabilizer of 14-3-3σ/ERα PPI complex with EC50 of 1 uM.
14-3-3σ/ERα stabilizer 181 shows remarkable selectivity for 14-3-3σ/ERα (appKD of 18 nM), with a similar selectivity profile as Fusicoccin-A (Cat# PC-61233).
14-3-3σ/ERα stabilizer 181 shows no stabilization of 14-3-3σ/C-RAF, SOS1, ChREBP, p65 and PIN1, up to 150 μM.
14-3-3σ/ERα stabilizer 181 shows a comparable stabilization profile as Fusicoccin-A.

Physicochemical Properties

M.Wt	496.47
Formula	C25H35Cl2N3O3
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
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Solubility	10 mM in DMSO
Chemical Name/SMILES	2-chloro-1-(9-(4-((4-chlorophenyl)amino)-2,6-dimethyltetrahydro-2H-pyran-4-carbonyl)-3,9-diazaspiro[5.5]undecan-3-yl)ethan-1-one

References

1. Konstantinidou M, et al. J Am Chem Soc. 2023 Sep 7. doi: 10.1021/jacs.3c05161.

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