Rheb inhibitor NR1
目录号: PL07576 纯度: ≥99%
CAS No. :2216763-38-9
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中文名称
Rheb inhibitor NR1
英文名称
Rheb inhibitor NR1
英文别名
Rheb inhibitor NR1;4-Bromo-6-((3,4-dichlorophenyl)thio)-1-(4-(dimethylcarbamoyl)benzyl)-1H-indole-2-carboxylic acid;4-bromo-6-[(3,4-dichlorophenyl)sulfanyl]-1-{[4-(dimethylcarbamoyl)phenyl]methyl}-1H-indole-2-carboxylic acid;NR1;BrC1=C2C=C(N(C2=CC(=C1)SC1=CC(=C(C=C1)Cl)Cl)CC1=CC=C(C=C1)C(N(C)C)=O)C(=O)O;E7V
Cas No.
2216763-38-9
分子式
C25H19BrCl2N2O3S
分子量
578.31
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Rheb inhibitor NR1 是一种 Rheb 抑制剂,IC50 为 2.1 μM。Rheb inhibitor NR1 可直接结合 Rheb switch II 结构域,选择性抑制 mTORC1 的激活。Rheb inhibitor NR1 抑制 mTORC1 驱动的 T389pS6K1 的磷酸化,并以剂量依赖的方式增加 S473pAKT 的磷酸化。Rheb inhibitor NR1 不影响 mTORC2 的活性。
生物活性
Rheb inhibitor NR1 is a Rheb inhibitor with an IC 50 of 2.1?μM in the Rheb-IVK assay. Rheb inhibitor NR1 can directly bind Rheb in the switch II domain and selectively inhibit the activation of mechanistic target of rapamycin complex 1 (mTORC1). Rheb inhibitor NR1 inhibits the phosphorylation of mTORC1 driven pS6K1 and increases the phosphorylation of pAKT in a dose-dependent manner. Rheb inhibitor NR1 does not influence mTORC2 activity.
性状
Solid
IC50 & Target[1][2]
Rheb, mTORC1
体外研究(In Vitro)
NR1 (1-10 μM; 48 h) reduces the size of Jurkat cells.
NR1 (0.37-30 μM; 90 min for MCF-7 and TRI102; 24 h for PC3) inhibits the phosphorylation of pS6K1 and increases the phosphorylation of pAKT in MCF-7, TRI102 and PC3 cells.
NR1 (1-30 μM; 2.5 h) reduced protein synthesis in MCF-7. has not independently confirmed the accuracy of these methods. They are for reference only.Cell Viability Assay
体内研究(In Vivo)
NR1 (30 mg/kg; IP; single dosage) significantly reduces mTORC1 activity in both kidney and skeletal muscle, and exhibited a clear band shift for 4E-BP1 in skeletal muscle. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Mahoney SJ, et al. A small molecule inhibitor of Rheb selectively targets mTORC1 signaling. Nat Commun. 2018 Feb 7;9(1):548.
溶解度数据
In Vitro: DMSO : 50 mg/mL (86.46 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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