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
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M.Wt
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860.73
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Formula
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C38H34F6N8O9
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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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
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References
1. Liu HY, et al. Nat Commun. 2024 Jun 19;15(1):5179.
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