Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GSK621 是一种特异性AMPK 激动剂,对 AML 细胞系的IC50值为13-30 μM。它可诱导自噬和凋亡,还可诱导eiF2α磷酸化。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 389 | 现货 | ||
5 mg | ¥ 995 | 现货 | ||
10 mg | ¥ 1,730 | 现货 | ||
25 mg | ¥ 3,580 | 现货 | ||
50 mg | ¥ 5,170 | 现货 | ||
100 mg | ¥ 7,280 | 现货 | ||
500 mg | ¥ 14,600 | 现货 |
产品描述 | GSK621 is a specific and potent AMPK activator. |
体外活性 | In AML cell lines and primary AML samples, GSK621 markedly increases phosphorylation at AMPKα T172, a marker of AMPK activation. In a set of 20 cell lines, GSK621 reduces the proliferation of all 20 lines with IC50 ranged from 13-30 μM, and increases apoptosis in 17 (85%) lines. In addition, GSK621 also triggers autophagy, which partially contributes to AML cell death. [1] |
体内活性 | In nude mice bearing MOLM-14 xenografts, GSK621 (30 mg/kg, i.p.) reduces leukemia growth and significantly extends survival by enhancing AMPK activity and the induction of apoptosis. [1] |
激酶实验 | AMPK enzymatic assay: HEPG2 cells are treated with increasing doses of A-769662 or GSK621, and ACC S79 phosphorylation is assessed as a surrogate marker for AMPK activation using a commercially available ELISA kit. |
细胞实验 | Twenty AML cell lines are treated with log10 dilutions of GSK621 and relative viability is determined by CellTiter-Glo?assay. IC50 of GSK621 among these 20 cell lines is calculated using the Prism software and are presented as log[C] with [C] in mol/l (M). Results are presented for 5 different cell lines per panel.(Only for Reference) |
分子量 | 489.91 |
分子式 | C26H20ClN3O5 |
CAS No. | 1346607-05-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 90 mg/mL (183.7 mM)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
H2O: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.0412 mL | 10.206 mL | 20.4119 mL | 51.0298 mL |
5 mM | 0.4082 mL | 2.0412 mL | 4.0824 mL | 10.206 mL | |
10 mM | 0.2041 mL | 1.0206 mL | 2.0412 mL | 5.103 mL | |
20 mM | 0.1021 mL | 0.5103 mL | 1.0206 mL | 2.5515 mL | |
50 mM | 0.0408 mL | 0.2041 mL | 0.4082 mL | 1.0206 mL | |
100 mM | 0.0204 mL | 0.1021 mL | 0.2041 mL | 0.5103 mL |
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。
GSK621 1346607-05-3 Apoptosis Autophagy Chromatin/Epigenetic PI3K/Akt/mTOR signaling AMPK CHOP inhibit AMP-activated protein kinase Inhibitor GSK-621 UPR PERK ATF4 GSK 621 ER Stress inhibitor