GSK_WRN3 | WRN helicase inhibitor | Probechem Biochemicals

Chemical Structure : GSK_WRN3

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GSK_WRN3 (WRNi, GSK-WRN3)

货号: PC-22109Not For Human Use, Lab Use Only.

GSK_WRN3 (WRNi, GSK-WRN3) is a potent and highly selective WRN helicase covalent inhibitor with biochemical pIC50 of 8.6, covalently targets WRN Cys727 residue.

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生物&药学活性

GSK_WRN3 (WRNi, GSK-WRN3) is a potent and highly selective WRN helicase covalent inhibitor with biochemical pIC50 of 8.6, covalently targets WRN Cys727 residue.
GSK_WRN3 displays exceptional specificity for WRN over other RecQ helicases (RecQ5, RecQ1, BLM), significantly modifies WRN Cys727 in Jurkat cells demonstrating the remarkable specificity.
GSK_WRN3 selectively inhibits microsatellite-unstable (MSI) cell growth in vitro and phenocopies genetic inactivation, induces cytotoxic chromosomal instability and DNA damage in MSI cancer cells, by selectively degrading WRN and concurrently upregulating DNA damage response markers such as p-ATM, p-KAP1, p21, and γ-H2AX.

物理化学性质&存储条件

分子量	352.41
分子式	C16H20N2O5S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(R)-6-cyclohexyl-N-(1,1-dioxido-2,3-dihydrothiophen-3-yl)-5-hydroxy-2-oxo-1,2-dihydropyridine-3-carboxamide

参考文献

1. Picco G, et al. Cancer Discov. 2024 Apr 9. doi: 10.1158/2159-8290.CD-24-0052.

GSK_WRN3 (WRNi, GSK-WRN3)

生物&药学活性

物理化学性质&存储条件

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GSK_WRN3 (WRNi, GSK-WRN3)

生物&药学活性

物理化学性质&存储条件

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