Powder: -20°C for 3 years | In solvent: -80°C for 1 year
RS6212 是一种特异性乳酸脱氢酶 (LDH) 抑制剂(IC50= 12.03 μM)。RS6212 在多种癌细胞系中显示出强大的抗癌活性。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
25 mg | ¥ 10,600 | 6-8周 | ||
50 mg | ¥ 13,800 | 6-8周 | ||
100 mg | ¥ 17,500 | 6-8周 |
产品描述 | RS6212 is a specific lactate dehydrogenase (LDH) inhibitor (IC50=12.03 μ M)。 RS6212 shows strong anticancer activity in a variety of cancer cell lines. |
体外活性 | Most cancer cells switch metabolism from mitochondrial oxidative phosphorylation to aerobic glycolysis, which is catalyzed by lactate dehydrogenase (LDH). Sonic Hedgehog (SHH) pathway aberrant activation is related to metabolism shifting to glycolysis [1]. RS6212 (compound 18) (80 μM; 0-72 h) exhibits significantly anti-proliferative activity against cancer cells and (1 μM, 10 μM, 100 μM; 24 h) inhibits Med-MB (SHH MB, medulloblastoma) with an IC 50 value of 81 μM [1]. RS6212 (80 μM; 6 h) decreases LDH activity, glycolytic level, and ECAR (extracellular acidification rate), and (12.03 μM; 6 h) increases NADH level [1]. RS6212 (0-320 μM; 48 h) inhibits cell growth in HCT116 cells without PARP cleavage nor LC3B–I lipidation [1]. RS6212 (50 nM and 100 nM; 24 h) increases inhibitory effect against HCT116 cells in combination with 50 nM or 100 nM rotenone. RS6212-Rotenone causes significant cleavage of PARP, thus activates programmed cell death of cancer cells [1]. Cell Proliferation Assay [1] Cell Line: HCT116 CRC cells lacking LDHA Concentration: 12.03 μM Incubation Time: 24 hours Result: Failed to inhibit cell proliferation without LDHA, indicating anticancer proliferation by specifically inhibiting LDHA activity. Cell Proliferation Assay [1] Cell Line: Hct116, SW480, A549, PANC-1 Concentration: 80 μM Incubation Time: 0, 24, 48, 72 hours Result: Inhibited cancer cells growth, characterized by increasing glycolytic metabolism. |
分子量 | 398.48 |
分子式 | C20H22N4O3S |
CAS No. | 2097925-52-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
RS6212 2097925-52-3 Inhibitor inhibitor inhibit