Cat. No.: HY-N1956

Rubiadin-1-methyl ether

1 Cited Publications

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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.

For research use only. We do not sell to patients.

Purity: 98.57%
CAS No.: 7460-43-7
Formula: C₁₆H₁₂O₄
Molecular Weight:268.26

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Rubiadin-1-methyl ether Chemical Structure

CAS No.: 7460-43-7

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

p65

All NF-κB Isoforms :

All TGF-β Receptor Isoforms :

In Vitro

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.

Cell Differentiation Assay^[1]

Cell Line:

Bone marrow-derived osteoclast precursors (OCPs)
Concentration:

0.1-10 mM
Incubation Time:

4 days
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.

Real Time qPCR^[1]

Cell Line:

Bone marrow-derived osteoclast precursors (OCPs)
Concentration:

0.1-10 mM
Incubation Time:

4 days
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.

In Vivo

Rubiadin-1-methyl ether (3-30 mg/kg; p.o.; single dose on day 14 post-induction) at 10 mg/kg exerts the most potent anti-pulmonary fibrosis efficacy, significantly reducing bleomycin-induced pulmonary inflammation, collagen deposition, and M2 macrophage polarization in mice^[2].
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.

Animal Model:

C57BL/6 (male, 10-12 weeks old, bleomycin-induced pulmonary fibrosis)^[2]
Dosage:

3 mg/kg; 10 mg/kg; 30 mg/kg
Administration:

p.o.; single dose (on day 14 post-induction)
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).

Animal Model:

Swiss mice (4-week-old male, 20-25 g, LPS-induced acute lung injury)^[3]
Dosage:

3 mg/kg; 10 mg/kg; 30 mg/kg
Administration:

p.o.; single dose 1 hour pre-LPS
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).

Chemical Information

CAS No. 7460-43-7
Appearance Solid
Molecular Weight 268.26
Formula C₁₆H₁₂O₄
Color Light yellow to yellow
SMILES

O=C1C2=C(C=CC=C2)C(C3=CC(O)=C(C)C(OC)=C13)=O
Structure Classification
- Quinones
- Anthraquinones
- Phenols
- Monophenols
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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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Sci Rep

Rubiadin-1-methyl ether alleviates bleomycin induced pulmonary fibrosis. [Abstract]

2026 Jan 8;16(1):4864. PMID: 41507413

Solvent & Solubility

In Vitro:

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.

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Concentration Solvent Mass

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5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.7277 mL

18.6386 mL

37.2773 mL

5 mM

0.7455 mL

3.7277 mL

7.4555 mL

10 mM

0.3728 mL

1.8639 mL

3.7277 mL

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.

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (287 KB)
SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
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- Portuguese - PT (392 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
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NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Rubiadin-1-methyl ether

1 Cited Publications

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Rubiadin-1-methyl ether

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Chemical Information

Publications (1)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Rubiadin-1-methyl ether Related Classifications

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