产品
编 号：F620445
分子式：C25H19BrCl2N2O3S
分子量：578.3
分子式：C25H19BrCl2N2O3S
分子量：578.3
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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结构图
CAS No: 2216763-38-9
产品详情
生物活性：
Rheb inhibitor NR1 is a Rheb inhibitor with an IC50 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 T389pS6K1 and increases the phosphorylation of S473pAKT in a dose-dependent manner. Rheb inhibitor NR1 does not influence mTORC2 activity.(Rheb-IVK: Rheb-dependent mTORC1 kinase activity)
体内研究：
NR1 (30 mg/kg；腹腔注射；单次剂量) 显著降低肾脏和骨骼肌中的 mTORC1 活性，并显示出骨骼肌中T37/464E-BP1 的明显带移。Animal Model:Male C57BL/6 mice (6-7 weeks; fast for 16 hours)
Dosage:30 mg/kg
Administration:IP; single dosage
Result:Sustained over 5?μM for 2?h.Significantly reduced mTORC1 activity in both kidney and skeletal muscle, and exhibited a clear band shift for T37/464E-BP1 in skeletal muscle.
体外研究：
NR1 (1-10 μM；48 小时) 减小 Jurkat 细胞的大小。 NR1 (0.37-30 μM；MCF-7 和 TRI102 90 分钟；24 小时PC3) 在 MCF-7、TRI102 和 PC3 细胞中抑制T389pS6K1 的磷酸化并增加S473pAKT 的磷酸化。 NR1 (1-30 μM；2.5 h) 减少 MCF-7中的蛋白质合成。
Rheb inhibitor NR1 is a Rheb inhibitor with an IC50 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 T389pS6K1 and increases the phosphorylation of S473pAKT in a dose-dependent manner. Rheb inhibitor NR1 does not influence mTORC2 activity.(Rheb-IVK: Rheb-dependent mTORC1 kinase activity)
体内研究：
NR1 (30 mg/kg；腹腔注射；单次剂量) 显著降低肾脏和骨骼肌中的 mTORC1 活性，并显示出骨骼肌中T37/464E-BP1 的明显带移。Animal Model:Male C57BL/6 mice (6-7 weeks; fast for 16 hours)
Dosage:30 mg/kg
Administration:IP; single dosage
Result:Sustained over 5?μM for 2?h.Significantly reduced mTORC1 activity in both kidney and skeletal muscle, and exhibited a clear band shift for T37/464E-BP1 in skeletal muscle.
体外研究：
NR1 (1-10 μM；48 小时) 减小 Jurkat 细胞的大小。 NR1 (0.37-30 μM；MCF-7 和 TRI102 90 分钟；24 小时PC3) 在 MCF-7、TRI102 和 PC3 细胞中抑制T389pS6K1 的磷酸化并增加S473pAKT 的磷酸化。 NR1 (1-30 μM；2.5 h) 减少 MCF-7中的蛋白质合成。
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