TRAM-34

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Chemical Structure| 289905-88-0 同义名 : Triarylmethane-34
CAS号 : 289905-88-0
货号 : A338045
分子式 : C22H17ClN2
纯度 : 98%
分子量 : 344.84
MDL号 : MFCD09842562
存储条件：

Pure form Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
靶点

  • Potassium Channel

    IKCa1 (KCa3.1), Kd:20 nM
描述 TRAM-34 is a highly selective blocker of intermediate-conductance calcium-activated K+ channel (IKCa1) (Kd=20 nM). TRAM-34 inhibits the cloned and the native IKCa1 channel in human T lymphocytes with a Kd of 20-25 nM and is 200- to 1,500-fold selective over other ion channels. Combinations of TRAM-34 and cyclosporin A are more effective in suppressing lymphocyte mitogenesis than either compound alone[3]. TRAM-34, a specific inhibitor of K(Ca)3.1 channels increased or decreased cell proliferation depending on the concentration. At intermediate concentrations (3-10 microM) TRAM-34 increased cell proliferation, whereas at higher concentrations (20-100 microM) TRAM-34 decreased cell proliferation. TRAM-34, as well as inhibiting K(Ca)3.1, directly interacts with the oestrogen receptor and mimics the effects of 17beta-oestradiol on MCF-7 cell proliferation and gene modulation[4]. TRAM-34 can inhibit the proliferation and invasion of HL-60 cells, and can induce cell apoptosis and G0/G1 arrest. The time and concentration of TRAM-34 have effect on the malignant behavior of HL-60 cells[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.90mL

0.58mL

0.29mL

14.50mL

2.90mL

1.45mL

29.00mL

5.80mL

2.90mL
参考文献

[1]Wang ZH, Shen B, et al. Blockage of intermediate-conductance-Ca(2+) -activated K(+) channels inhibits progression of human endometrial cancer. Oncogene. 2007 Aug 2;26(35):5107-14.

[2]Wulff H, Miller MJ, et al. Design of a potent and selective inhibitor of the intermediate-conductance Ca2+-activated K+ channel, IKCa1: a potential immunosuppressant. Proc Natl Acad Sci U S A. 2000 Jul 5;97(14):8151-6.

[3]Wulff H, Miller MJ, Hansel W, Grissmer S, Cahalan MD, Chandy KG. Design of a potent and selective inhibitor of the intermediate-conductance Ca2+-activated K+ channel, IKCa1: a potential immunosuppressant. Proc Natl Acad Sci U S A. 2000 Jul 5;97(14):8151-6

[4]Roy JW, Cowley EA, Blay J, Linsdell P. The intermediate conductance Ca2+-activated K+ channel inhibitor TRAM-34 stimulates proliferation of breast cancer cells via activation of oestrogen receptors. Br J Pharmacol. 2010 Feb 1;159(3):650-8

[5]Jiang TH, Huang ZG. [Effects of TRAM-34 on Proliferation and Invasion of Leukemia Cell Line HL-60]. Zhongguo Shi Yan Xue Ye Xue Za Zhi. 2017 Feb;25(1):104-109. Chinese