GSK621
作者：齐岳
发布时间：2023-09-14
09:03:56
点击数：
产品名称：GSK621
产品描述：
| 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 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 90 mg/mL (183.7 mM)
Ethanol: <1 mg/mL
H2O: <1 mg/mL
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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