GSK621
| CAS号 | 1346607-05-3 | 货号 | BCP31970 |
| 中文名 | GSK621 | ||
| 英文名 | GSK621 | ||
| 中文别名 | |||
| 英文别名 | GSK-621; GSK 621; | ||
| 分子式 | C26H20ClN3O5 | 分子量 | 489.91 |
| 生物活性 | GSK621 is a potent and selective AMPK agonist. GSK621 selectively kills acute myeloid leukemia (AML) cells but spares normal hematopoietic progenitors. This differential sensitivity results from a unique synthetic lethal interaction involving concurrent activation of AMPK and mTORC1. Strikingly, the lethality of GSK621 in primary AML cells and AML cell lines is abrogated by chemical or genetic ablation of mTORC1 signaling. Cytotoxicity in AML cells from GSK621 involves the eIF2α/ATF4 signaling pathway that specifically results from mTORC1 activation. AMPK activation may represent a therapeutic opportunity in mTORC1-overactivated cancers. | ||
| 信号通路 | PI3K/Akt/mTOR Epigenetics | ||
| 靶 点 | AMPK | ||
结构式
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