| 应用 |
An ATP-competitive DNA-PK, PI 3-kinase, and FRAP inhibitor. |
| 产品介绍 |
PI-103是一种多靶点的PI3K抑制剂，对p110α的抑制效果最好，IC50为2 nM (对p110β/δ/γ抑制效果稍弱)，也抑制mTORC1/2和DNA-PK ，IC50分别为20 nM/83 nM和8 nM。 |
| 备注 |
PI-103 is a multi-targeted PI3K inhibitor for p110α/β/δ/γ with IC50 of 2 nM/3 nM/3 nM/15 nM, less potent to mTOR/DNA-PK with IC50 of 30 nM/23 nM. |
| 生化机理 |
PI-103 is a cell-permeable pyridinylfuranopyrimidine compound that acts as an ATP-competitive inhibitor of DNA-PK, PI 3-kinase (Class IA), and FRAP (mTOR) complex 1 and 2. Studies suggest that PI-103 can induce apoptosis and an arrest in the cell cycle by inhibition of the aforementioned proteins. When PI-103 is combined with rapamycin, a prototypic mTORC1 inhibitor, synergistic suppression of AKT and ribosomal S6 protein phosphorylation are observed. In addition, PI-103 has been seen to have nominal effects inhibiting basal Na+ transport, but is very effective in abolishing insulin-induced Na+ absorption in the nephron. |
| 别名 |
PI 103 ; 3-[4-(4-吗啉基吡啶并[3',2',4,5]呋喃并[3,2-d]嘧啶-2-基]苯酚;PI 103;PI103;PI 3-K Inhibitor V;3-[4-(4-Morpholinylpyrido[3',2',4,5]furo[3,2-d]pyrimidin-2-yl]phenol |
