TRAM-34

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A membrane-permeable blocker of IKCa1/KCa3.1 (Kds = 20 and 25 nM for the cloned and native channel in COS-7 cells and human T lymphocytes, respectively); 200- to 1,500-fold selective for IKCa1 over Kv (Kv1.1-Kv1.5, Kv3.1, Kv4.2), Kir2.1, BK/KCa1.1, SKCa (rSKCa2, hSKCa2, hSKCa3), native SKCa/KCa2, and CRAC in Jurkat T cells as well as sodium and chloride channels; suppresses reactivation of human-derived T lymphocytes stimulated with anti-CD3 antibody (mean EC50s = 295 and 910 nM from sensitive and less sensitive human donors, respectively); inhibits proliferation of human endometrial cancer cells and induces cell cycle arrest at the G0/G1 phase; inhibits proliferation of LNCaP and PC3 prostate cancer cells; inhibits proliferation induced by epidermal growth factor (EGF) in smooth muscle A7r5 cells (IC50 = 8 nM); reduces intimal hyperplasia by approximately 40% after 1, 2, and 6 weeks in a rat model of balloon catheter injury when administered at a dose of 120 mg/kg per day; pretreatment of HEC-1-A cells with TRAM-34 at a concentration of 30 µM inhibits tumor growth in vivo in nude mice