CW-069 is an allosteric inhibitor of microtubule motor protein HSET with an IC50 of 75 μM.
体外研究
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.
分子式
C23H21In2O3
分子量
500.33
CAS号
1594094-64-0
运输条件
Room temperature in continental US; may vary elsewhere.