PROTAC survivin degrader-1 is an orally active, CNS-penetrant survivin -targeting PROTAC. PROTAC survivin degrader-1 induces degradation of survivin via the ubiquitin proteasome system. PROTAC survivin degrader-1 can be used for the research of glioblastoma [1]. (Pink: Survivin ligand; Blue: Cereblon ligand; Black: linker).
In Vitro, PROTAC survivin degrader-1 (compound 11) (0.03-3 μM; 24 h) reduces survivin protein levels in U87 and CL261 glioblastoma cells[1]. PROTAC survivin degrader-1 (0.01-1.0 μM; 48 h) induces a DNA damage response in GL261 glioblastoma cells and potentiates the DNA damage, cell killing, and apoptotic effects of 2Gy irradiation[1]. PROTAC survivin degrader-1 (0.5 μM; 2 weeks) potentiates the cytotoxic effect of 0Gy, 2Gy, 4Gy, 6Gy, and 8Gy irradiation in GL261 glioblastoma cells[1]. PROTAC survivin degrader-1 (10-100 nM; 24 h) induces proteasome-dependent survivin degradation in U87 glioblastoma cells[1].
References:
[1]. Shuhua Zheng, et al. Survivin-targeted compounds. WO2025063888A1.
In Vitro, PROTAC survivin degrader-1 (compound 11) (0.03-3 μM; 24 h) reduces survivin protein levels in U87 and CL261 glioblastoma cells[1]. PROTAC survivin degrader-1 (0.01-1.0 μM; 48 h) induces a DNA damage response in GL261 glioblastoma cells and potentiates the DNA damage, cell killing, and apoptotic effects of 2Gy irradiation[1]. PROTAC survivin degrader-1 (0.5 μM; 2 weeks) potentiates the cytotoxic effect of 0Gy, 2Gy, 4Gy, 6Gy, and 8Gy irradiation in GL261 glioblastoma cells[1]. PROTAC survivin degrader-1 (10-100 nM; 24 h) induces proteasome-dependent survivin degradation in U87 glioblastoma cells[1].
References:
[1]. Shuhua Zheng, et al. Survivin-targeted compounds. WO2025063888A1.