WRN-IN-26 is an orally active Werner syndrome helicase (WRN) inhibitor with a human K i value of 58.7 μM and an IC 50 value of 0.026 μM. WRN-IN-26 selectively targets the cysteine residues of WRN. WRN-IN-26 induces the expression of p21 protein in MSI-H tumor cells. WRN-IN-26 inhibits the growth of MSI-H tumor cells and exhibits potent in vivo efficacy in MSI-H xenograft tumor models. WRN-IN-26 can be used for the research of microsatellite instability-high (MSI-H) cancers.
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