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GSK_WRN4 is a covalent inhibitor of the DNA helicase Werner syndrome protein (WRN; IC50 = 25 nM).1 It inhibits tumor growth and increases intratumoral levels of the DNA damage markers p21, phosphorylated γH2AX, and phosphorylated KAP-1 in an SW48 colorectal cancer mouse xenograft model when administered at a dose of 300 mg/kg.
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