| 应用 |
A highly potent, ATP-competitive, and specific mTOR kinase inhibitor |
| 产品介绍 |
WYE-125132是ATP竞争性mTOR选择性抑制剂，IC50为0.19 nM，对PI3Ks及其相关的hSMG1和ATR抑制性较弱。 |
| 生化机理 |
WYE-125132 is a potent, ATP-competitive inhibitor of recombinant mTOR kinase,with an IC50 of 0.19 nM. WYE-125132 shows an anti-proliferative activity against a variety of tumor cell lines with IC50 ranging from 2 nM (LNCap) to 380 nM (HTC116), in vitro. WYE-125132 causes inhibition of protein synthesis and cell size, induction of apoptosis, and cell cycle progression. WYE-125132 causes pre-tRNA Leu synthesis reduction by 72%, 80%, and 53% in actively proliferating cells of MG63, MDA361, and HEK293, respectively as a result of the inhibition of mTORC1. WYE-125132 induces Maf1 dephosphorylation and its accumulation in the nucleus. |
| 别名 |
WYE-125132；WYE 125132; WYE125132；WYE 125132; N-[4-[1-(1,4-二氧杂螺[4.5]癸烷-8-基)-4-(8-氧杂-3-氮杂双环[3.2.1]辛烷-3-基)-1H-吡唑并[3,4-d]嘧啶-6-基]苯基]-N'-甲基脲;WYE-125132；WYE 125132;WYE125132；N-[4-[1-(1,4-Dioxaspiro[4.5]dec-8-yl)-4-(8-oxa-3-azabicyclo[3.2.1]oct-3-yl)-1H-pyrazolo[3,4-d]pyrimidin-6-yl]phenyl]-N'-methylurea |
