475988
mTOR抑制剂III，PP242
The mTOR Inhibitor III, PP242 controls the biological activity of mTOR. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
别名:
mTOR抑制剂III，PP242, 2-（4-氨基-1-异丙基-1H-吡唑并[3，4-d]嘧啶-3-基）-1H-吲哚-5-醇，二水合物，TORKinib，mTOR抑制剂III，PP242
产品名称
mTOR抑制剂III，PP242, The mTOR Inhibitor III, PP242 controls the biological activity of mTOR. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
color
off-white
storage condition
protect from light
OK to freeze
assay
≥97% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
solubility
DMSO: 100 mg/mL
shipped in
wet ice
storage temp.
−20°C
Quality Level
相关类别
Disclaimer
毒性：标准处理（A）
General description
一种可渗透细胞的吡唑并嘧啶化合物，可作为两种mTORC1 &mTORC2的有效，可逆和ATP竞争性抑制剂（分别为IC50 = 30 &58 nM，具有100 µM ATP）。PP242抑制PKCα，p110γ和JAK2的效价降低6倍，13倍和14倍，并且在1 µM的浓度下对一组216种其他激酶的活性大大降低或没有活性（分别用10或100 µM ATP观察到最大抑制为68%或77%）。PP242在体外培养物（2.5µ M）和小鼠体内（20 mg/kg i.p.）中差异抑制胰岛素刺激的细胞蛋白磷酸化，其方式与在mTORC2功能敲除SIN1-/-细胞中或在用雷帕霉素（目录号 553210，553211，553212）处理的培养物中观察到的方式明显不同，其仅靶向mTORC1，而不靶向mTORC2。 在初级MEF中胰岛素刺激后，PP242阻断4EBP1 T36/T45/S65磷酸化与帽结合蛋白eIF4E增强的4EBP1关联性密切相关，从而选择性抑制了帽依赖性而非帽非依赖性蛋白翻译。
Other Notes
Feldman, M.E., et al. 2009.PLoS Biology7, 391.
Apsel, B., et al. 2008.Nat. Chem. Biol.4, 691.
Apsel, B., et al. 2008.Nat. Chem. Biol.4, 691.
Packaging
用惰性气体包装
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
存储类别
11 - Combustible Solids
wgk
WGK 2
flash_point_f
Not applicable
flash_point_c
Not applicable
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