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GSK_WRN3

Chemical Structure : GSK_WRN3

CAS No.: 2923009-50-9

GSK_WRN3 (WRNi, GSK-WRN3)

Catalog No.: 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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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

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.

Physicochemical Properties

M.Wt 352.41
Formula C16H20N2O5S
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

(R)-6-cyclohexyl-N-(1,1-dioxido-2,3-dihydrothiophen-3-yl)-5-hydroxy-2-oxo-1,2-dihydropyridine-3-carboxamide

References

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

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