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
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所有图片(1)
About This Item
经验公式（希尔记法）:
C16H16N6O · 2H2O
分子量:
344.37
UNSPSC代码:
12352200
NACRES:
NA.77
质量水平
检测方案
≥97% (HPLC)
形式
solid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
颜色
off-white
溶解性
DMSO: 100 mg/mL
运输
wet ice
储存温度
−20°C
一般描述
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。
包装
用惰性气体包装
警告
毒性：标准处理（A）
其他说明
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.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
WGK
WGK 2
闪点(°F)
Not applicable
闪点(°C)
Not applicable
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