Rubiadin-1-methyl ether
Based on 1 publication(s) in Google Scholar
Rubiadin-1-methyl ether is an orally potent NF-κB p65 inhibitor and autophagy inhibitor. Rubiadin-1-methyl ether inhibits RANKL-induced phosphorylation and nuclear translocation of p65, suppresses BECN1 transcription, blocks LC3 conversion and autophagosome formation, thereby reducing the levels of BECN1 mRNA and Beclin1 protein. Rubiadin-1-methyl ether inhibits osteoclastogenesis, cell proliferation, macrophage M2 polarization and the TGF-β1 signaling pathway, and effectively alleviates pulmonary inflammation. Rubiadin-1-methyl ether is widely used in research on osteoporosis, pulmonary fibrosis, idiopathic pulmonary fibrosis, acute lung injury and other related diseases.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.57%
- CAS 番号: 7460-43-7
- 分子式: C16H12O4
- 分子量:268.26
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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MedChemExpress（MCE）の使用を引用している文献 Rubiadin-1-methyl ether
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生物活性
製品説明
IC50 & Target
[1]|
p65 |
体外実験
Rubiadin-1-methyl ether (0.1-10 mM; 6, 12, 24 h) inhibits the proliferation of bone marrow-derived osteoclast precursors (OCPs) in a concentration-dependent manner when incubated for 6, 12, or 24 h in the presence of RANKL and M-CSF[1].
Rubiadin-1-methyl ether (0.1-10 mM; 4 days) inhibits RANKL- and M-CSF-induced differentiation of bone marrow-derived osteoclast precursors (OCPs) into mature and large osteoclasts in a concentration-dependent manner after 4 days of incubation[1].
Rubiadin-1-methyl ether (0.1-10 mM; 4 days) downregulates the mRNA expression of osteoclast-related genes (CTSK, MMP9, TRAP) in bone marrow-derived osteoclast precursors (OCPs) in a concentration-dependent manner after 4 days of incubation with RANKL and M-CSF[1].
Rubiadin-1-methyl ether (0.1-10 mM; 12 h) inhibits RANKL-induced LC3 conversion (a marker of autophagy) in bone marrow-derived osteoclast precursors (OCPs) in a concentration-dependent manner after 12 h of incubation[1].
Rubiadin-1-methyl ether (0.1-10 mM; 12 h) inhibits RANKL-induced p65 phosphorylation in bone marrow-derived osteoclast precursors (OCPs) in a concentration-dependent manner after 12 h of incubation[1].
Rubiadin-1-methyl ether (10 mM; 12 h) inhibits RANKL-induced LC3 conversion and LC3-puncta formation (markers of autophagy) in bone marrow-derived osteoclast precursors (OCPs) after 12 h of incubation, and this effect is reversed by the Beclin1 activator TAT-Beclin1[1].
Rubiadin-1-methyl ether (10 mM; 12 h) reverses RANKL-induced p65 nuclear translocation in bone marrow-derived osteoclast precursors (OCPs) after 12 h of incubation, restoring cytoplasmic p65 levels to ~0.92-fold and reducing nuclear p65 levels to ~0.91-fold relative to control[1].
Rubiadin-1-methyl ether (10 mM; 12 h) reduces RANKL-induced BECN1 mRNA and Beclin1 protein expression in bone marrow-derived osteoclast precursors (OCPs) after 12 h of incubation, and this effect is reversed by the Beclin1 activator TAT-Beclin1[1].
Rubiadin-1-methyl ether (10 mM; 12 h) reduces RANKL-induced BECN1 mRNA and Beclin1 protein expression in bone marrow-derived osteoclast precursors (OCPs) after 12 h of incubation, and this effect is reversed by p65 overexpression[1].
Rubiadin-1-methyl ether (10 mM; 12 h) inhibits RANKL-induced LC3 conversion and LC3-puncta formation (markers of autophagy) in bone marrow-derived osteoclast precursors (OCPs) after 12 h of incubation, and this effect is reversed by p65 overexpression[1].
Rubiadin-1-methyl ether (1-300 μM; 24 h) has low cytotoxicity in RAW 264.7 murine macrophages, with a CC10 of 30 μM[3].
Rubiadin-1-methyl ether (3-30 μM; 24 h LPS stimulation) at 30 μM reverses the LPS-induced decrease in apoptosis rate in RAW 264.7 murine macrophages[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Bone marrow-derived osteoclast precursors (OCPs)
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Concentration:0.1-10 mM
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Incubation Time:4 days
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Result:Inhibited the number and size of mature osteoclasts in a concentration-dependent manner.
Reduced the number of mature osteoclasts per well to ~160 with 0.1 mM RBM, ~80 with 1 mM RBM, and ~30 with 10 mM RBM, compared to ~230 in the control group.
Reduced the number of large osteoclasts per well to ~55 with 0.1 mM RBM, ~20 with 1 mM RBM, and ~10 with 10 mM RBM, compared to ~110 in the control group.
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Cell Line:Bone marrow-derived osteoclast precursors (OCPs)
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Concentration:0.1-10 mM
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Incubation Time:4 days
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Result:Reduced the mRNA expression levels of osteoclast-related genes in a concentration-dependent manner.
Reduced CTSK mRNA expression to ~0.8-fold with 0.1 mM RBM, ~0.7-fold with 1 mM RBM, and ~0.4-fold with 10 mM RBM, compared to control.
Reduced MMP9 mRNA expression to ~0.6-fold with 0.1 mM RBM, ~0.4-fold with 1 mM RBM, and ~0.3-fold with 10 mM RBM, compared to control.
Reduced TRAP mRNA expression to ~0.9-fold with 0.1 mM RBM, ~0.8-fold with 1 mM RBM, and ~0.7-fold with 10 mM RBM, compared to control.
体内実験
Rubiadin-1-methyl ether (3-30 mg/kg; p.o.; single dose 1 hour pre-LPS) exerts dose-dependent anti-inflammatory and immunomodulatory effects in LPS-induced acute lung injury in mice, with the highest dose of 30 mg/kg producing the most robust reductions in leukocyte infiltration, proinflammatory mediator levels, and lung tissue damage, alongside increased IL-10 production[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (male, 10-12 weeks old, bleomycin-induced pulmonary fibrosis)[2]
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Dosage:3 mg/kg; 10 mg/kg; 30 mg/kg
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Administration:p.o.; single dose (on day 14 post-induction)
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Result:Ameliorated bleomycin-induced weight loss, reduced elevated lung coefficient, attenuated lung tissue pathological damage, reduced Ashcroft fibrosis score, decreased BALF total inflammatory cells by ~47.2% (neutrophils by ~59.4%, lymphocytes by ~25.6%), downregulated lung mRNA expression of fibrosis-associated genes Fn1 by ~52.4%, Col1a1 by ~30.8%, and Acta2 by ~44.3%, reduced lung M2 macrophage (F4/80+CD206+) proportion from 28.4% to 19.8%, downregulated lung mRNA expression of M2-related genes Mrc1 by ~48.3%, Arg1 by ~46.1%, Tgfb1 by ~59%, and Il10 by ~38.7%, reduced BALF levels of TGF-β1 by ~28.7%, IL-6 by ~26.5%, IL-1β by ~55%, and TNF-α by ~51% (10 mg/kg dose).
Showed no significant reduction in total inflammatory cells, with efficacy not statistically significant compared to the bleomycin group (3 mg/kg dose).
Reduced BALF total inflammatory cells by ~49.6% (neutrophils by ~61.2%, lymphocytes by ~28.7%) with no statistical difference compared to the 10 mg/kg group, showed no additional improvement in efficacy compared to the 10 mg/kg group, with a trend toward inferior results in some measures (30 mg/kg dose).
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Animal Model:Swiss mice (4-week-old male, 20-25 g, LPS-induced acute lung injury)[3]
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Dosage:3 mg/kg; 10 mg/kg; 30 mg/kg
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Administration:p.o.; single dose 1 hour pre-LPS
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Result:Decreased total leukocyte count in BALF by 43.6% (10 mg/kg) and 55.3% (30 mg/kg).
Reduced neutrophil migration by 48.1% (10 mg/kg) and 68.8% (30 mg/kg).
Reduced lung fluid leakage (protein content in BALF) by 55.5% (3 mg/kg), 81.9% (10 mg/kg), and 82.9% (30 mg/kg).
Decreased NOx levels in BALF by 46.3% (3 mg/kg), 51.8% (10 mg/kg), and 60.1% (30 mg/kg).
Reduced myeloperoxidase (MPO) activity by 41.8% (3 mg/kg), 50.1% (10 mg/kg), and 54.7% (30 mg/kg).
Reduced IL-12p70 levels by 37.1% (3 mg/kg), 47.4% (10 mg/kg), and 79.5% (30 mg/kg).
Reduced IL-6 levels by 33.7% (3 mg/kg), 49% (10 mg/kg), and 79.5% (30 mg/kg).
Reduced IFN-γ levels by 64.5% (10 mg/kg) and 88.4% (30 mg/kg).
Reduced TNF-α levels by 27.7% (10 mg/kg) and 69.2% (30 mg/kg).
Reduced MCP-1 levels by 82.6% (30 mg/kg).
Increased anti-inflammatory IL-10 levels by 324.8% (10 mg/kg) and 360.5% (30 mg/kg).
Reduced lung injury histological scores by 43.4% (30 mg/kg).
化学情報
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CAS 番号 7460-43-7
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性状 Solid
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分子量 268.26
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分子式 C16H12O4
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Color Light yellow to yellow
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SMILES
O=C1C2=C(C=CC=C2)C(C3=CC(O)=C(C)C(OC)=C13)=O
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Structure Classification
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Initial Source
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Sci Rep
2026 Jan 8;16(1):4864. PMID: 41507413
溶剤 & 溶解度
体外:
DMSO : ≥ 125 mg/mL (465.97 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (287 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Cai S, et al. Rubiadin-1-methyl ether inhibits BECN1 transcription and Beclin1-dependent autophagy during osteoclastogenesis by inhibiting NF-κB p65 activation. Exp Biol Med (Maywood). 2023;248(17):1518-1526. [Content Brief]
[2]. Zhen X, et al. Rubiadin-1-methyl ether alleviates bleomycin induced pulmonary fibrosis. Sci Rep. 2026;16(1):4864. Published 2026 Jan 8. [Content Brief]
[3]. Mohr ETB, et al. Evidence That the Anti-Inflammatory Effect of Rubiadin-1-methyl Ether Has an Immunomodulatory Context. Mediators Inflamm. 2019;2019:6474168. Published 2019 Nov 3. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.7277 mL | 18.6386 mL | 37.2773 mL | 93.1932 mL |
| 5 mM | 0.7455 mL | 3.7277 mL | 7.4555 mL | 18.6386 mL | |
| 10 mM | 0.3728 mL | 1.8639 mL | 3.7277 mL | 9.3193 mL | |
| 15 mM | 0.2485 mL | 1.2426 mL | 2.4852 mL | 6.2129 mL | |
| 20 mM | 0.1864 mL | 0.9319 mL | 1.8639 mL | 4.6597 mL | |
| 25 mM | 0.1491 mL | 0.7455 mL | 1.4911 mL | 3.7277 mL | |
| 30 mM | 0.1243 mL | 0.6213 mL | 1.2426 mL | 3.1064 mL | |
| 40 mM | 0.0932 mL | 0.4660 mL | 0.9319 mL | 2.3298 mL | |
| 50 mM | 0.0746 mL | 0.3728 mL | 0.7455 mL | 1.8639 mL | |
| 60 mM | 0.0621 mL | 0.3106 mL | 0.6213 mL | 1.5532 mL | |
| 80 mM | 0.0466 mL | 0.2330 mL | 0.4660 mL | 1.1649 mL | |
| 100 mM | 0.0373 mL | 0.1864 mL | 0.3728 mL | 0.9319 mL |
Rubiadin-1-methyl ether 関連分類
HY-N1956 関連分類
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