| 应用 |
An ATP-competetive mTOR (FRAP) inhibitor |
| 产品介绍 |
WAY-600 is a potent, ATP-competitive and selective inhibitor of mTOR with IC50 of 9 nM; blocks mTORC1/P-S6K(T389) and mTORC2/P-AKT(S473) but not P-AKT(T308); selective for mTOR than PI3Kα (>100-fold) and PI3Kγ (>500-fold). |
| 生化机理 |
WAY-600 is a potent ATP-competitive mTOR inhibitor with an IC50 of about 9 nM. It is well reported that the mammalian target of rapamycin (sc-3504) (mTOR also known as FRAP) is centrally involved in cell growth, metabolism, and angiogenesis. WAY-600 has significant selectivity against mTOR (FRAP) over phosphatidylinositol 3-kinase (PI3K) isofoms (>100-fold). WAY-600 treated HEK293 cells indicated a 50% inhibition of polysomes by Way-600 compared with the 11% suppression by rapamycin. Unlike the rapalogs,WAY-600 acutely blocked mTORC2-dependent phosphorylation of AKT in vitro. In various cancer cells, WAY-600 inhibited the mTORC1 substrate P-S6K(T389) and mTORC2 substrate P-AKT(S473) at submicromolar concentrations without significant inhibition of P-AKT(T308). |
| 别名 |
WAY 600；6-(1H-吲哚-5-基)-4-(4-吗啉基)-1-[1-(3-吡啶基甲基)-4-哌啶基]-1H-吡唑并[3,4-d]嘧啶;WAY 600；6-(1H-Indol-5-yl)-4-(4-morpholinyl)-1-[1-(3-pyridinylmethyl)-4-piperidinyl]-1H-pyrazolo[3,4-d]pyrimidine |
