Rheb inhibitor NR1是一种小分子，可抑制单体蛋白Rheb，IC50值为2.1μM。
Cas No.:2216763-38-9
Sample solution is provided at 25 µL, 10mM.
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Rheb inhibitor NR1 is a small molecule that inhibits the monomeric protein Rheb with an IC50 value of 2.1μM [1]. Rheb inhibitor NR1 targets the switch II domain of Rheb1 via hydrophobic interactions, specifically inhibiting mTORC1 activity [2]. Rheb inhibitor NR1 has been widely used to promote cell survival under conditions of glucose deprivation [3].
In vitro, Treatment of PK-15 cells with 30μM Rheb inhibitor NR1 for 12 hours significantly reduced the replication of foot-and-mouth disease virus (FMDV) in the cells[4]. Treatment with Rheb inhibitor NR1 (10μM) for 24 hours significantly inhibited the expression of OTUD4 and GPX4 in HEK293T cells[5].
In vivo, Rheb inhibitor NR1 treatment (1mg/kg; three times a week; i.p.) combined with NSC23766 for 2 weeks attenuated hearing dysfunction in Tnfaip8l2−/− mice and improved the disordered arrangement of stereocilia[6].
References:
[1] Mahoney S J, Narayan S, Molz L, et al. A small molecule inhibitor of Rheb selectively targets mTORC1 signaling[J]. Nature communications, 2018, 9(1): 548.
[2] Rahman M, Nguyen T M, Lee G J, et al. Unraveling the role of ras homolog enriched in brain (Rheb1 and Rheb2): bridging neuronal dynamics and cancer pathogenesis through mechanistic target of rapamycin signaling[J]. International Journal of Molecular Sciences, 2024, 25(3): 1489.
[3] Li M, Huang W, Zhang Y, et al. Glucose deprivation triggers DCAF1-mediated inactivation of Rheb-mTORC1 and promotes cancer cell survival[J]. Cell Death & Disease, 2024, 15(6): 409.
[4] Liu H, Zhu Z, Xue Q, et al. Picornavirus infection enhances aspartate by the SLC38A8 transporter to promote viral replication[J]. PLoS pathogens, 2023, 19(2): e1011126.
[5] Chen J, Huang C, Mei J, et al. OTUD4 inhibits ferroptosis by stabilizing GPX4 and suppressing autophagic degradation to promote tumor progression[J]. Cell Reports, 2025, 44(5).
[6] Li W, Li Y, Wang M, et al. TNFAIP8L2 maintains hair cell function and regulates age-related hearing loss via mTORC1 signaling[J]. Molecular Therapy, 2025, 33(7): 3036-3055.
Rheb inhibitor NR1是一种小分子，可抑制单体蛋白Rheb，IC50值为2.1μM[1]。Rheb inhibitor NR1通过疏水相互作用靶向Rheb1的开关II结构域，特异性抑制mTORC1活性[2]。Rheb inhibitor NR1已被广泛用于在葡萄糖剥夺条件下促进细胞存活[3]。
在体外，用30μM的Rheb inhibitor NR1处理PK-15细胞12小时，可显著减少口蹄疫病毒（FMDV）在细胞中的复制[4]。用Rheb inhibitor NR1（10μM）处理HEK293T细胞24小时，显著抑制了OTUD4和GPX4的表达[5]。
在体内，Rheb inhibitor NR1（1mg/kg；每周三次；腹腔注射）联合NSC23766治疗2周，可减轻Tnfaip8l2−/−小鼠的听力功能障碍，并改善静纤毛的紊乱排列[6]。
| Cell experiment [1]: | |
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Cell lines |
HEK293T cells |
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Preparation Method |
HEK293T cells were cultured in high-glucose Dulbecco’s Modified Eagle Medium (DMEM) supplemented with 10% fetal bovine serum (FBS) in a humidified atmosphere containing 5% CO2 at 37°C. Cells were passaged every 2-3 days to maintain stable growth conditions. Cells were treated for 24h with Erastin, chloroquine (50μM), rapamycin (10μM), 3-Methyladenine (1mM), and Rheb inhibitor NR1 (10μM), and western blot analysis was carried out. |
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Reaction Conditions |
10μM; 24h |
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Applications |
Rheb inhibitor NR1 treatment significantly inhibited the expression of OTUD4 and GPX4 in HEK293T cells. |
| Animal experiment [2]: | |
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Animal models |
Tnfaip8l2−/− mice |
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Preparation Method |
Tnfaip8l2−/− mice were kept in temperature-controlled (21°C-25°C) and humidity-maintained (40%-70%) rooms with a 12h light/dark cycle. Water and food were provided freely. Mice in the intervention group received i.p. injections of either rapamycin at a dose of 2mg/kg or a combined administration of Rheb inhibitor NR1 and NSC23766 at a dose of 1mg/kg three times a week for 2 consecutive weeks. Control mice received i.p. injections of DMSO. Analyze the hearing function of mice. |
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Dosage form |
1mg/kg; three times a week for 2 weeks; i.p. |
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Applications |
Rheb inhibitor NR1 treatment combined with NSC23766 attenuated hearing dysfunction in Tnfaip8l2−/− mice. |
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References: |
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| Cas No. | 2216763-38-9 | SDF | |
| Canonical SMILES | O=C(C(N1CC2=CC=C(C(N(C)C)=O)C=C2)=CC3=C1C=C(SC4=CC=C(Cl)C(Cl)=C4)C=C3Br)O | ||
| 分子式 | C25H19BrCl2N2O3S | 分子量 | 578.3 |
| 溶解度 | DMSO: 100 mg/mL (172.92 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.7292 mL | 8.646 mL | 17.2921 mL |
| 5 mM | 345.8 μL | 1.7292 mL | 3.4584 mL |
| 10 mM | 172.9 μL | 864.6 μL | 1.7292 mL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
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2.
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