2. NF-κB Autophagy TGF-beta/Smad
  3. NF-κB RANKL/RANK Autophagy TGF-β Receptor
  4. Rubiadin-1-methyl ether

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.

Rubiadin-1-methyl ether

Rubiadin-1-methyl ether Chemical Structure

CAS No. : 7460-43-7

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
1 mg In-stock
5 mg In-stock
10 mg In-stock
50 mg   Get quote  
100 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Rubiadin-1-methyl ether Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Rubiadin-1-methyl ether

View All NF-κB Isoform Specific Products:

View All Isoforms
NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

View All TGF-β Receptor Isoform Specific Products:

View All Isoforms
ALK1 ALK2 ALK3 ALK4 ALK5 ALK6 ALK7 TGFβR2 ACVR2A ACVR2B BMP

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1][2][3].

IC50 & Target[1]

p65

 

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.

Rubiadin-1-methyl ether Related Antibodies

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).
Molecular Weight

268.26

Formula

C16H12O4
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1C2=C(C=CC=C2)C(C3=CC(O)=C(C)C(OC)=C13)=O
Structure Classification
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
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.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.7277 mL 18.6386 mL 37.2773 mL
5 mM 0.7455 mL 3.7277 mL 7.4555 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 98.57%

SDS (392 KB)

COA (252 KB) HNMR (244 KB) LCMS (105 KB)

Handling Instructions (2659 KB)
References

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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

Rubiadin-1-methyl ether Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Rubiadin-1-methyl ether7460-43-7NF-κBRANKL/RANKAutophagyTGF-β ReceptorNuclear factor-κBNuclear factor-kappaBTransforming growth factor beta receptorsBECN1RANKLpulmonary fibrosisBeclin1RAW 264.7 murine macrophagesbone marrow-derived osteoclast precursorsLC3osteoclastogenesisNF-κB p65autophagyInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Rubiadin-1-methyl ether
Cat. No.:
HY-N1956
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

English - EN (392 KB) Français - FR (392 KB) Deutsch - DE (392 KB) Norwegian - NO (392 KB) Español - ES (392 KB) Swedish - SV (392 KB) Italian - IT (392 KB) Korean - KR (392 KB) Portuguese - PT (392 KB)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.