Name | TRAM-34 |
Description | TRAM-34 (Triarylmethane-34) (Kd=20 nM), an effective and specific inhibitor of the intermediate-conductance Ca2+-activated K+ channel (IKCa1, KCa3.1), does not block cytochrome P450. The selective activity of TRAM-34(TRAM 34) is 200 to 1500-fold than other ion channels. |
Cell Research | Cells are exposed to TRAM-34 for 48 hours. After 48 hours, cells are harvested by suction (suspension cells) or by trypsinization (adherent cell lines), centrifuged, resuspended in 0.5 mL PBS containing 1 μg/mL propidium iodide (PI), and red fluorescence measured on a FACScan flow cytometer. The percentage of dead cells is determined by their PI uptake, 104 cells of every sample being analyzed. (Only for Reference) |
Kinase Assay | Electrophysiology: The human IKCa1 is cloned and expressed in COS-7 cells. Cells are studied in the whole-cell configuration of the patch-clamp technique. The holding potential is 280 mV. The internal pipette solution contains: 145 mM K+ aspartate, 2 mM MgCl2, 10 mM Hepes, 10 mM K2EGTA, and 8.5 mM CaCl2 (1 μM free Ca2+), pH 7.2, 290-310 mOsm. To reduce currents from the native chloride channels in COS-7 cells, Na+ aspartate Ringer is used as an external solution: 160 mM Na+ aspartatey/4.5 mM KCl/2 mM CaCl2/1 mM MgCl2/5 mM Hepes, pH 7.4/290-310 mOsm. IKCa currents in COS-7 cells are elicited by 200-ms voltage ramps from -120 mV to 40 mV applied every 10 seconds and the reduction of slope conductance at -80 mV by TRAM-34 taken as a measure of channel block. |
In vitro | 与克霉唑不同,TRAM-34选择性地抑制IKCa1,而不阻断细胞色素P450酶(CYP3A4)。TRAM-34在IKCa1转染的COS-7细胞中以及人类T淋巴细胞和T84细胞中的天然IKCa电流上,比克霉唑更强效地抑制克隆IKCa1通道。TRAM-34展现出对其他离子通道,如KV、BKCa、SKCa、Na+、CRAC和Cl-通道。TRAM-34显著地以295-910 nM和85-830 nM的IC50,分别抑制抗CD3 Ab或PKC激活剂PMA加钙离子载体离子霉素诱导的人类T淋巴细胞激活。5 μM的TRAM-34不影响人类T淋巴细胞或几种细胞线的细胞活力。[1] TRAM-34显著抑制EGF诱导的IKCa1上调,并以8 nM的IC50,抑制A7r5细胞的EGF刺激的增殖。[2] TRAM-34处理抑制人类子宫内膜癌(EC)细胞的增殖,并阻断EC细胞周期在G0/G1期。[3] |
In vivo | TRAM-34以约500-1,000倍于阻断剂量(0.5 mg/kg/day)的剂量连续治疗7天,对小鼠无毒性。[1] 以120 mg/kg/day的剂量给予TRAM-34能显著减少约40%的大鼠气球导管损伤(BCI)模型中的内膜增生。[2] 与其体外抑制EC细胞增殖的作用一致,30 μM的TRAM-34治疗能够减缓HEC-1-A肿瘤在体内的发展。[3] |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | DMSO : 3.5 mg/mL (10 mM), Heating is recommended.
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Keywords | TRAM-34 | Inhibitor | Potassium Channel | KcsA | inhibit | TRAM34 |
Inhibitors Related | Tetraethylammonium chloride | Amlexanox | Cloperastine hydrochloride | Quinine | Resveratrol | 2,2,2-Trichloroethanol | Minoxidil sulfate | Tetraethylammonium bromide | Indapamide | (±)-Naringenin | Butamben | Halothane |
Related Compound Libraries | Inhibitor Library | Anti-Breast Cancer Compound Library | Bioactive Compound Library | Bioactive Compounds Library Max | Potassium Channel Targeted Library | Anti-Aging Compound Library | HIF-1 Signaling Pathway Compound Library | Ion Channel Targeted Library | Membrane Protein-targeted Compound Library | Pain-Related Compound Library |