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2-12-2-deg

Chemical Structure : 2-12-2-deg

CAS No.:

2-12-2-deg

Catalog No.: PC-22558Not For Human Use, Lab Use Only.

2-12-2-deg is a PROTAC targeting the dengue virus (DENV) envelope (E) protein with DC50 of 0.21 uM, Dmax of 95%, depletes intracellular E via a CRBN- and proteasome-dependent mechanism.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

2-12-2-deg is a PROTAC targeting the dengue virus (DENV) envelope (E) protein with DC50 of 0.21 uM, Dmax of 95%, depletes intracellular E via a CRBN- and proteasome-dependent mechanism.
2-12-2-deg exhibits increased antiviral potency compared to the parental E inhibitor 2-12-2, with EC90 WT value of 1.67 uM, and 13.27 uM respectively.
2-12-2-deg has a dual mode of action: inhibition of E's function in viral entry and blocking of viral particle production due to a targeted protein degradation (TPD) mechanism.
2-12-2-deg exhibits broad-spectrum activity against multiple flaviviruses, with antiviral EC90 values consistently in the single-digit micromolar across ZIKV, JEV, and WNV Kunjin.

Physicochemical Properties

M.Wt 860.73
Formula C38H34F6N8O9
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

N-(2-(2-(2-((2-(2-imino-6-oxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)oxy)ethoxy)ethoxy)ethyl)-3-(trifluoromethoxy)-4-((4-((4-(trifluoromethoxy)phenyl)amino)pyrimidin-2-yl)amino)benzamide

References

1. Liu HY, et al. Nat Commun. 2024 Jun 19;15(1):5179.

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