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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。


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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 | 库存 | 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 |
GSK621 相关产品
| 产品描述 | GSK621 is a specific and potent AMPK activator. |
| 体外活性 | 在AML细胞系和初级AML样本中,GSK621显著增强了AMPKα T172位点的磷酸化,这是AMPK激活的标志。在一组20个细胞系中,GSK621抑制了所有20个细胞系的增殖,IC50范围为13-30 μM,并在17个(占85%)细胞系中增加了凋亡。此外,GSK621还触发了自噬,这部分促成了AML细胞的死亡。[1] |
| 体内活性 | 在裸鼠体内携带MOLM-14异种移植物的实验中,GSK621(30 mg/kg, i.p.)通过增强AMPK活性和诱导凋亡,有效降低了白血病的生长速度并显著延长了生存期。[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 |
| Smiles | COc1cccc(c1)-n1c(=O)[nH]c2cc(Cl)n(-c3ccc(cc3)-c3cccc(OC)c3O)c2c1=O |
| 密度 | 1.41 g/cm3 (Predicted) |
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| 溶解度信息 | DMSO: 90 mg/mL (183.71 mM), Sonication is recommended. Ethanol: < 1 mg/mL (insoluble or slightly soluble) H2O: < 1 mg/mL (insoluble or slightly soluble) | |||||||||||||||||||||||||||||||||||
| 体内实验配方 | 10% DMSO+90% Corn Oil: 1 mg/mL (2.04 mM), Sonication is recommeded. 请按顺序添加溶剂,在添加下一种溶剂之前,尽可能使溶液澄清。如有必要,可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考,体内配方并不是绝对的,请根据不同情况进行调整。 | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
DMSO
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