Clofilium-tosylate - Potassium Channel Blocker - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEClofilium tosylateCat. No.: HY-33350CAS No.: 92953-10-1分式: CHClNOS分量: 510.17作靶点: Potassium Channel; Apoptosis作通路: Membrane Transporter/Ion Channel; Apoptosis储存式: 4C, protect from light* In solvent : -80C, 6 months; -20C, 1 month

2、 (protect fromlight)溶解性数据体外实验 DMSO : 125 mg/mL (245.02 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 1.9601 mL 9.8007 mL 19.6013 mL5 mM 0.3920 mL 1.9601 mL 3.9203 mL10 mM 0.1960 mL 0.9801 mL 1.9601 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验 请根据您的实验动物和给药式选择适当的溶解案，配制前请

3、先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (4.08 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (4.08 mM); Clear solution3.

4、 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (4.08 mM); Clear solution1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 Clofilium tosylate种钾通道 (potassium channel) 阻滞剂，作于早幼粒细胞病 (HL-60) 细胞，激活 caspase-3 诱导凋亡。具有抗律失常作 1。IC50 & Target Potassium channel 1体外研究 HL-60 cells tr

5、eated with Clofilium (0-20 M; 24, 48, and 72 hours) lead to suppression of viability andproliferation in both time and concentration-dependent manners. Cell viability decreases significantly in HL-60 cells treated with 2.5 M to 10 M of Clofilium 1.Clofilium (10 M, 12 hours) induces the proteolytic c

6、leavage of inactive procaspase-3, p34 into its activeform, p17 and subsequent cleavage of its substrate PARP at 2 h after exposure to 10 mM Clofilium.However, there is no significant change in expression of Bcl-2 and Bax proteins 1.Cell Viability Assay 1Cell Line: HL-60 cellsConcentration: 0-20 MInc

7、ubation Time: 24, 48, and 72 hoursResult: Inhibited HL-60 cells with IC50s of 6.3 M for 24 hours, 3.4 M for 48 hours, 2.4 M for72 hours, respectively.Western Blot Analysis 1Cell Line: HL-60 cellsConcentration: 10 MIncubation Time: 12 hoursResult: Induced proteolytic cleavage of caspase-3 and subsequ

8、ent cleavage of its substrate,PARP, while Bcl-2 and Bax proteins were unaltered.REFERENCES1. Choi BY, et al. Clofilium, a potassium channel blocker, induces apoptosis of human promyelocytic leukemia (HL-60) cells via Bcl-2-insensitive activation of caspase-3. Cancer Lett. 1999 Dec 1;147(1-2):85-93.McePdfHeightCaution: Product has not been fully validated for medical applications