Chemical Structure : WRN degrader 14c
货号: 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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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.
| 分子量 | 727.84 | |
| 分子式 | C37H44F3N5O5S | |
| 外观性状 | Solid | |
| 储存条件 |
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| Solubility |
10 mM in DMSO |
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1. Tao W, et al. Eur J Med Chem. 2025 Sep 4;300:118121.
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