| 应用 |
A selective FRAP inhibitor |
| 产品介绍 |
Torkinib (PP242)是一种选择性的mTOR抑制剂，IC50为8 nM；靶向作用于mTOR复合体，作用于mTOR比作用于PI3Kδ或PI3Kα/β/γ选择性分别高10倍多和100倍。 |
| 备注 |
PP242 is a selective mTOR inhibitor with IC50 of 8 nM; targets both mTOR complexes with >10- and 100-fold selectivity for mTOR than PI3Kδ or PI3Kα/β/γ, respectively. |
| 生化机理 |
PP242 has been shown to be a an ATP-competitive mTORC1/mTORC2 (FRAP) inhibitor (IC50 = 8 nM). PP242 is the first selective inhibitor that targets the ATP domain of FRAP. This compound shows selectivity for FRAP over other PI 3K family kinases (IC50 values are 0.102, 0.408, 1.27, 1.96 and 2.2 μM for p110γ, DNA-PK, p110δ, p110α and p110β respectively). Furthermore, PP242 hydrate inhibits both S6K and 4EBP1 phosphorylation this activity displays an overall decrease in cap-dependent protein translation. |
| 别名 |
PP 242; PP-242;2-(4-氨基-1-异丙基-1H-吡唑并[3,4-d]嘧啶-3-基)-1H-吲哚-5-醇;2-(4-amino-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-1H-indol-5-ol;Torkinib |
