Bardoxolone Methyl

Catalog No.S8078

Bardoxolone Methyl is an IKK inhibitor, showing potent proapoptotic and anti-inflammatory activities. Phase 3.

Price Stock Quantity  
USD 97 In stock
USD 570 In stock
Bulk Inquiry

Massive Discount Available

Free Overnight Delivery on all orders over $ 500.

Bardoxolone Methyl Chemical Structure

Bardoxolone Methyl Chemical Structure
Molecular Weight: 505.69

Validation & Quality Control

1 customer reviews :

Quality Control & MSDS

Product Information

  • Compare IκB/IKK Inhibitors
    Compare IκB/IKK Products
  • Research Area

Product Description

Biological Activity

Description Bardoxolone Methyl is an IKK inhibitor, showing potent proapoptotic and anti-inflammatory activities. Phase 3.
Targets IKK [3]
(Cell-free assay)
In vitro Bardoxolone Methyl exhibits potent inhibitory activities against production of nitric oxide induced by interferon-Ƴ in mouse macrophages with IC50 of 0.1 nM. [1] Bardoxolone Methyl decreases the viability of leukemic HL-60, KG-1, and NB4 cells with IC50 of 0.4, 0.4, and 0.27 μM, respectively. CDDO-Me induces pro-apoptotic Bax protein, inhibits the activation of ERK1/2, and it blocks Bcl-2 phosphorylation, which contributes to the induction of apoptosis. [2] Bardoxolone Methyl potently inhibits both constitutive and inducible NF-kappaB activated by TNF, interleukin (IL)-1beta, phorbol ester, okadaic acid, hydrogen peroxide, lipopolysaccharide, and cigarette smoke. [3]
In vivo Bardoxolone Methyl (60 mg/kg) reduces the number, size, and severity of lung tumors in vivo. [4] Bardoxolone Methyl significantly reduces the in vivo inflammatory cytokine response following LPS challenge, induces HO-1 protein expression in the spleen, and protects mice against lethal-dose LPS. [5]
Features The only IKKβ inhibitor in clinical use for solid tumors, type 2 diabetes, and chronic kidney disease. An orally-available antioxidant inflammation modulator.

Protocol(Only for Reference)

Kinase Assay:


IKK assay To determine the effect of CDDO-Me on TNF-induced IKK activation, IKK is analyzed. Briefly, the IKK complex from whole-cell extracts was precipitated with antibody against IKKα and IKKβ and then treated with protein A/G-Sepharose beads. After 2 hours, the beads are washed with lysis buffer and then resuspended in a kinase assay mixture containing 50 mmol/L HEPES (pH 7.4), 20 mmol/L MgCl2, 2 mmol/L DTT, 20 μCi [γ-32P]ATP, 10 μmol/L unlabeled ATP, and 2 μg of substrate glutathione S-transferase-IκBα (amino acids 1-54). After incubation at 30°C for 30 minutes, the reaction is terminated by boiling with SDS sample buffer for 5 minutes. Finally, the protein is resolved on 10% SDS-PAGE, the gel is dried, and the radioactive bands are visualized with a Storm820. To determine the total amounts of IKK-α and IKK-β in each sample, 50 μg of whole-cell proteins are resolved on 7.5% SDS-PAGE, electrotransferred to a nitrocellulose membrane, and then blotted with either anti-IKK-α or anti-IKK-β antibody.

Cell Assay:


Cell lines HL-60, KG-1, and NB4 cells
Concentrations ~5 μM
Incubation Time 72 hours

Leukemic cell lines are cultured at a density of 3.0 × 105 cells/mL, and AML mononuclear cells are cultured at 5 × 105 cells/mL in the presence or absence of indicated concentrations of CDDO-Me. Appropriate amounts of DMSO (final concentration less than 0.05%) are included as control. For cytotoxicity studies, 1 μM ara-C is added to the cultures. After 24 to 72 hours, viable cells are counted with the trypan blue dye exclusion method using a hematocytometer.

Animal Study:


Animal Models Female A/J mice are injected i.p. with vinyl carbamate.
Formulation DMSO
Dosages ~60 mg/kg
Administration Oral gavage

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)
Body Surface Area (m2)0.0070.0250.
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)


[1] Honda T, et al. J Med Chem. 2000, 43(22), 4233-4246.

[2] Konopleva M, et al. Blood. 2002, 99(1), 326-335.

view more

Clinical Trial Information( data from, updated on 2016-07-30)

NCT Number Recruitment Conditions Sponsor
Start Date Phases
NCT02657356 Not yet recruiting Connective Tissue Disease-Associated Pulmonary Arterial Hypertension Reata Pharmaceuticals, Inc. September 2016 Phase 3
NCT02316821 Recruiting Chronic Kidney Disease|Type 2 Diabetes Kyowa Hakko Kirin Company, Limited December 2014 Phase 2
NCT02036970 Recruiting Pulmonary Arterial Hypertension|Pulmonary Hypertension Reata Pharmaceuticals, Inc. May 2014 Phase 2
NCT01655186 Withdrawn Renal Insufficiency, Chronic|Diabetes Mellitus, Type 2 Reata Pharmaceuticals, Inc. September 2012 Phase 2
NCT01689116 Completed Healthy Volunteers Reata Pharmaceuticals, Inc. August 2012 Phase 1

view more

Chemical Information

Download Bardoxolone Methyl SDF
Molecular Weight (MW) 505.69


CAS No. 218600-53-4
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms RTA 402, TP-155, NSC 713200, CDDO Methyl Ester
Solubility (25°C) * In vitro DMSO 21 mg/mL (41.52 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo 4% DMSO+30% PEG 300+5% Tween+ddH2O 5mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name Oleana-1,9(11)-dien-28-oic acid, 2-cyano-3,12-dioxo-, methyl ester

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

* Indicates a Required Field

Related IκB/IKK Products

  • WS3

    WS3 is a β cell proliferation inducer via modulation of Erb3 binding protein-1 (EBP1) and the IκB kinase pathway.

  • LY2409881

    LY2409881 is a potent and selective IKK2 inhibitor with IC50 of 30 nM, >10-fold selectivity over IKK1 and other common kinases.

  • AZD3264

    AZD3264 is a novel IKK2 inhibitor.

  • BAY 11-7082

    BAY 11-7082 is a NF-κB inhibitor, inhibits TNFα-induced IκBα phosphorylation with IC50 of 10 μM in tumor cells. Also inhibiting components of the ubiquitin system.

  • IKK-16 (IKK Inhibitor VII)

    IKK-16 (IKK Inhibitor VII) is a selective IκB kinase (IKK) inhibitor for IKK-2, IKK complex and IKK-1 with IC50 of 40 nM, 70 nM and 200 nM in cell-free assays, respectively.

  • BMS-345541

    BMS-345541 is a highly selective inhibitor of the catalytic subunits of IKK-2 and IKK-1 with IC50 of 0.3 μM and 4 μM in cell-free assays, respectively.

  • IMD 0354

    IMD-0354 is an IKKβ inhibitor and blocks IκBα phosphorylation in NF-κB pathway.

  • TPCA-1

    TPCA-1 is an inhibitor of IKK-2 with IC50 of 17.9 nM in a cell-free assay, inhibits NF-κB pathway, exhibits 22-fold selectivity over IKK-1.

  • Bay 11-7085

    BAY 11-7085 is an irreversible inhibitor of TNFα-induced IκBα phosphorylation with IC50 of 10 μM.

  • SC-514

    SC-514 is an orally active, ATP-competitive IKK-2 inhibitor with IC50 of 3-12 μM, blocks NF-κB-dependent gene expression, does not inhibit other IKK isoforms or other serine-threonine and tyrosine kinases.

Recently Viewed Items

Tags: buy Bardoxolone Methyl | Bardoxolone Methyl supplier | purchase Bardoxolone Methyl | Bardoxolone Methyl cost | Bardoxolone Methyl manufacturer | order Bardoxolone Methyl | Bardoxolone Methyl distributor
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Contact Us