tcsc2329 CW-069

CW-069 is an allosteric inhibitor of HSET with an IC₅₀ of 75 μM.

IC50 & Target: IC50: 75 μM (HSET)^[1]

In Vitro: CW-069 is an allosteric inhibitor of HSET with an IC₅₀ of 75 μM. CW-069 shows statistically significant selectivity over KSP. CW-069 potently suppresses N1E-115 cells, and less potently inhibits the NHDF cells, with IC₅₀ of 86 ± 10 μM and 181 ± 7 μM, respectively. CW-069 (100 or 200 μM) causes increased multipolar spindles in N1E-115 cells with supernumerary centrosomes and shows no effect on altering bipolar spindle morphology in normal human dermal fibroblast cells. CW-069 (200 μM) cacuses multipolar anaphase and cell death induced in N1E-115 cells via transfection with HSET siRNA, and antagonizes inhibition of KSP by monastrol, but does not exert mitotic arrest in HeLa cells^[1].