Werner syndrome RecQ helicase-IN-4 is a potent and orally active werner syndrome recQ helicase (WRN) inhibitor with an IC50 value of 0.06 µM. Werner syndrome RecQ helicase-IN-4 shows antiproliferative activity. Werner syndrome RecQ helicase-IN-4 shows anticancer activity.
Werner syndrome RecQ helicase-IN-4 (example 58) (0-10 µM; 8-20 days) shows antiproliferative activity with GI50s of 0.07, >10 µM for SW48, DLD1 WRN-KO cells, respectively[1].
Werner syndrome RecQ helicase-IN-4 (240 mg/kg; daily for 18 days) shows anticancer activity in mouse[1].
References:
[1]. Vincent Bordas, et al. Triazolo-pyrimidine analogues for treating diseases connected to the inhibiton of werner syndrome recq helicase (wrn). WO2022249060A1.