Chemical Structure : WRN degrader 14c
CAS No.:
3095277-20-3
WRN degrader 14c
(LdCHT 14c)
Catalog No.: PC-25461Not For Human Use, Lab Use Only.
WRN degrader 14c is a potent, selective degrader of Werner syndrome helicase (WRN) with DC50 of 1.7 uM in MSI-H HCT116 cells, covalently conjugates to C727 within the WRN helicase domain, forming an adamantane-tagged adduct that initiates sustained proteasomal degradation.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
WRN degrader 14c is a potent, selective degrader of Werner syndrome helicase (WRN) with DC50 of 1.7 uM in MSI-H HCT116 cells, covalently conjugates to C727 within the WRN helicase domain, forming an adamantane-tagged adduct that initiates sustained proteasomal degradation.
WRN degrader 14c induces potent, highly selective and sustained WRN degradation, outperforming the parental inhibitor H3B-219, with negligible impact on other tested proteins even at 25 uM.
WRN degrader 14c induces WRN degradation through the ubiquitin proteasome system.
WRN degrader 14c exhibits superior antiproliferative and antimetastatic efficacy than H3B-219.
WRN degrader 14c induces significant apoptosis, cell cycle arrest and DNA damage in HCT-116 cells.
Physicochemical Properties
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M.Wt
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727.84
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Formula
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C37H44F3N5O5S
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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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References
1. Tao W, et al. Eur J Med Chem. 2025 Sep 4;300:118121.
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