Tamoxifen-PEG-Clozapine

Tamoxifen-PEG-Clozapine (0.03-100 μM; 24 h) significantly reduces the ERα protein level in MCF-7 breast cancer cells after 24 h of incubation at concentrations of 30 μM and 100 μM, whereas it slightly increases the ERα level at lower concentrations (0.03-10 μM)^[1].
Tamoxifen-PEG-Clozapine (30 μM; 24 h) significantly reduces the ERα protein level in MCF-7 breast cancer cells, an effect that cannot be achieved by equimolar concentrations of 4-OHT (HY-16950A), Clozapine (HY-14539), or their combination^[1].
The ERα-degrading effect of Tamoxifen-PEG-Clozapine (30-100 μM; 24 h) in MCF-7 breast cancer cells is completely blocked by co-treatment with the proteasome inhibitor MG132 (HY-13259) or the ubiquitin-activating enzyme inhibitor MLN7243 (HY-100487), confirming that this degradation process is dependent on the ubiquitin-proteasome system^[1].
Tamoxifen-PEG-Clozapine inhibits the viability of MCF-7 breast cancer cells in a concentration-dependent manner, and this effect is associated with its ERα degradation activity^[1].

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