OUP-186

OUP-186 is a high affinity and human/rat species-selective antagonist of histamine H3 receptor. OUP-186 suppressed the proliferation of breast cancer cells. The IC50 values at 48 hours for OUP-186 was approximately 50 μM. OUP-186 potently induced cell death by activating caspase-3/7. In addition, OUP-186 treatment blocked the proliferation increase triggered by 100 μM (R)-(-)-α-methylhistamine (H3R agonist). OUP-186 potently suppresses proliferation and induces caspase-dependent apoptotic death in both ER+ and ER-breast cancer cells.