| 產(chǎn)品描述： | Torkinib (PP 242) is a selective and ATP-competitive mTOR inhibitor with an IC50 of 8 nM. PP242 inhibits both mTORC1 and mTORC2 with IC50s of 30 nM and 58 nM, respectively |
| 靶點(diǎn)： |
mTORC1:30 nM (IC50);mTORC2:58 nM (IC50);mTOR:8 nM (IC50);p110δ:100 nM (IC50);DNA-PK:410 nM (IC50);PDGFR:410 nM (IC50);p110α:2 μM (IC50);p110β:2.2 μM (IC50);p110γ:1.3 μM (IC50);Abl:3.6 μM (IC50);Hck:1.2 μM (IC50);Scr:1.4 μM (IC50);Scr(T338I):5.1 μM (IC50);VEGFR2:1.5 μM (IC50);EGFR:4.4 μM (IC50);EphB4:3.4 μM (IC50);Autophagy;Mitophagy;Apoptosis;Mitophagy;PI3K;mTOR;Autophagy |
| 體內(nèi)研究： |
In fat and liver, Torkinib (PP 242) is able to completely inhibit the phosphorylation of Akt at S473 and T308, consistent with its effect on these phosphorylation sites observed in cell culture. Surprisingly, Torkinib (PP 242) is only partially able to inhibit the phosphorylation of Akt in skeletal muscle and is more effective at inhibiting the phosphorylation of T308 than S473, despite it's ability to fully inhibit the phosphorylation of 4EBP1 and S6. These results will be confirmed by in vivo dose-response experiments, but, consistent with the partial effect of Torkinib (PP 242) on pAkt in skeletal muscle, a muscle-specific knockout of the integral mTORC2 component rictor resulted in only a partial loss of Akt phosphorylation at S473. These results suggest that a kinase other than mTOR, such as DNA-PK, may contribute to phosphorylation of Akt in muscle |
| 參考文獻(xiàn)： |
1. Apsel B, et al. Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. Nat Chem Biol. 2008 Nov;4(11):691-9. 2. Feldman ME, et al. Active-site inhibitors of mTOR target rapamycin-resistant outputs of mTORC1 and mTORC2. PLoS Biol. 2009 Feb 10;7(2):e38. |
| 溶解性： |
DMSO : 50 mg/mL (162.16 mM; Need ultrasonic) |
| 保存條件： |
2-8℃ |
| 配置溶液濃度參考： |
|
1mg |
5mg |
10mg |
| 1 mM |
3.243 ml |
16.216 ml |
32.432 ml |
| 5 mM |
0.649 ml |
3.243 ml |
6.486 ml |
| 10 mM |
0.324 ml |
1.622 ml |
3.243 ml |
| 50 mM |
0.065 ml |
0.324 ml |
0.649 ml |
|
| 注意： |
部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。 |
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