PROTAC KSP degrader 1

PROTAC KSP degrader 1 (Compound 21) (30 min) inhibits basal KSP ATPase activity in cell-free biochemical assays, with an IC₅₀ of 290.20 nM^[1].
PROTAC KSP degrader 1 (50-1000 nM; 48 h) dose-dependently degrades KSP in HCT-116 cells, with a DC₅₀ of 114.8 nM and a D_max of 90%. It also time-dependently degrades KSP within 48 h, and this degradation is mediated by the ubiquitin-proteasome system^[1].
PROTAC KSP degrader 1 (72 h) potently inhibits the proliferation of HCT-116 cells with an IC₅₀ value of 10.2 nM; it also exhibits moderate antiproliferative activity against A549, MCF-7 and MDA-MB-231 cells, with corresponding IC₅₀ values of 160.5 nM, 423.9 nM and 35.4 nM^[1].
PROTAC KSP degrader 1 (10-100 nM; 24 h) induces G₂/M phase cell cycle arrest in HCT-116 cells in a dose-dependent manner in vitro. After treatment with 10 nM and 100 nM for 24 h, the proportions of cells in the G₂/M phase reach 14.79% and 75.05%, respectively^[1].
PROTAC KSP degrader 1 (10-100 nM; 48 h) induces apoptosis in HCT-116 cells in a dose-dependent manner. After treatment with 10 nM and 100 nM for 48 h, the proportions of apoptotic cells are 28.47% and 55.90%, respectively^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.