Dual mTORC1/mTORC2 inhibitor
PP 242 is an ATP-competitive mTORC1/mTORC2 inhibitor (IC50 = 8 nM). Displays selectivity for mTOR 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) and 215 further kinases. Displays modest inhibition of PKCα, JAK2, PKCβI, PKCβII and RET (IC50 values are 0.049, 0.110, 0.185, 0.198 and 0.224 μM respectively). Inhibits both S6K and 4EBP1 phosphorylation; activity causes a decrease in cap-dependent protein translation. Also triggers downregulation of cFLIPS and augments TRAIL-induced apoptosis of cancer cells. PP 242 also inhibits oncogenic K-Ras and PI 3-K induced lipogenesis in breast cancer cells.
| Marque | Tocris |
|---|---|
| Réf. B-LABO | BL-RE-151359 |
| Réf. fabricant | 18707446 |
| Nom chimique ou matériau | 2-[4-Amino-1-(1-methylethyl)-1H-pyrazolo[3,4-d]pyrimidin-3-yl]-1H-indol-5-ol |
| CAS | 1092351-67-1 |
| Plage de pourcentage du dosage | >98% |
| Quantité | 5 mg |
| Formule moléculaire | C<sub>16</sub>H<sub>16</sub>N<sub>6</sub>O |
| Poids de la formule | Observed MW: 308.34 |
