KWR137 is a novel potent inhibitor of Werner protein WRN with IC50 of 8 nM (WRN ATPase).
KWR137 is more potent than HRO761 on WRN ATPase activity, but slightly weaker effect on WNR helicase activity.
KWR137 exhibits a GI50 value of 0.352 μM in SW48 cells.
KWR137 induces WRN degradation in the MSI-H CRC cells, SW48 and HCT116, but caused no degradation in the MSS CRC cell line, SW620. KWR137 (40 mg/kg, oral, daily) exhibits significant antitumor effects in SW48 cell xenograft model mice.
