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Chemical Structure : 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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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.
| M.Wt | 352.41 | |
| Formula | C16H20N2O5S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Picco G, et al. Cancer Discov. 2024 Apr 9. doi: 10.1158/2159-8290.CD-24-0052.
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