Torkinib (PP242)

    • 货号:MC0523
      • CasNo:
      • 1092351-67-1
      • 分子式:
      • C16H16N6O
      • 纯度:
      • >98%
      • 靶点:
      • mTOR
      • IC50:
      • IC50: 8 nM (mTOR), 100 nM (p110δ), 410 nM (DNA-PK), 410 nM (PDGFR)[1]
      • 体外研究:
      • PP 242 (PP242) potently inhibits mTOR (IC50=8 nM) but is much less active against other PI3K family members. Testing of PP 242 against 219 protein kinases reveals remarkable selectivity relative to the protein kinome: at a concentration 100-fold above its IC50 for mTOR, PP 242 inhibits only one kinase by more than 90% (Ret) and only three by more than 75% (PKCα, PKCβII and JAK2V617F)[1]. PP 242 (PP242) has a dose-dependent effect on proliferation and at higher doses is much more effective than Rapamycin at blocking cell proliferation. The ability of PP 242 to block cell proliferation more efficiently than Rapamycin could be a result of its ability to inhibit mTORC1 and mTORC2, because Rapamycin can only inhibit mTORC1. In SIN1-/- MEFs, Rapamycin is also less effective at blocking cell proliferation than PP 242. That PP 242 and Rapamycin exhibit very different anti-proliferative effects in SIN1-/- MEFs suggests that the two compounds differentially affect mTORC1[2].
      • 体内研究:
      • In fat and liver, PP 242 (PP242) 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, 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 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[2].
      • 简介:
      • 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; also showed slightly weaker activity against BRD4 (Kd= 1.7 uM).
      • 特异性:
      • TargetTargets both mTOR complexes with >10- and 100-fold selectivity for mTOR than PI3Kδ or PI3Kα/β/γ, respectively; also showed slightly weaker activity against BRD4 (Kd= 1.7 uM).
      • 稀释:
      • IC50: 8 nM (mTOR), 100 nM (p110δ), 410 nM (DNA-PK), 410 nM (PDGFR)[1]
      • 浓度:
      • >98%
      • 储存:
      • 2 years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO
      • 其他名称:
      • TORKinib,PP242; PP-242,PP 242
      • 分子量:
      • 308.34
      • 产品图片