Product Data SheetProduct Name:CAS No.: CatNo:Cat. No.:MWt:Formula:Purity :TRAM-342905-88-0HY-13519HY13519344.84C22H17ClN2>98%Solubility:DMSO04mg/ml;Water<1mg/mlDMSO 0.4 mg/ml; Water <1 mg/mlMechanisms: Pathways:Membrane Tranporter/Ion Channel; Target:PotassiunChannel Biological Activity:TRAM-34 is a highly selective blocker of intermediate conductance Ca2+-activated K+ channels(KCa3.1) (Kd = 20 nM). IC50 value: 20 nM (Kd) [1] Target: KCa3.1 in vitro: TRAM-34 inhibits the cloned and the native IKCa1 channel in human T lymphocytes with aK(d) of 20-25 nM and is 200- to 1,500-fold selective over other ion channels. Using TRAM-34, weshow that blocking IKCa1 in human lymphocytes, in the absence of P450-inhibition, results insuppression of mitogen-stimulated [(3)H]thymidine incorporation of preactivated lymphocytes withEC(50)valuesof100nM1microMdependingonthedonor[1]TRAM34aspecificinhibitorofEC(50)-values of 100 nM-1 microM depending on the donor [1]. TRAM-34, a specific inhibitor ofK(Ca)3.1 channels increased or decreased cell proliferation depending on the concentration. Atintermediate concentrations (3-10 microM) TRAM-34 increased cell proliferation, whereas at higherconcentrations (20-100 microM) TRAM-34 decreased ce...References:[1]. Wulff H, et al. Design of a potent and selective inhibitor of the intermediate-conductance Ca2+-activatedK+channelIKCa1:apotentialimmunosuppressantProcNatlAcadSciUSA2000Julactivated K+ channel, IKCa1: a potential immunosuppressant. Proc Natl Acad Sci U S A. 2000 Jul5;97(14):8151-6. [2]. Roy JW, et al. The intermediate conductance Ca2+-activated K+ channel inhibitor TRAM-34stimulates proliferation of breast cancer cells via activation of oestrogen receptors. Br J Pharmacol.2010 Feb 1;159(3):650-8. [3]. Chen YJ, et al. The KCa3.1 blocker TRAM-34 reduces infarction and neurological deficit in a ratmodel of ischemia/reperfusion stroke. J Cereb Blood Flow Metab. 2011 Dec;31(12):2363-74. Caution: Not fully tested. For research purposes onlyMedchemexpress LLCwww.medchemexpress.com18Wilkinson Way, Princeton, NJ 08540,USAEmail: info@medchemexpress.com Web: www.medchemexpress.com
