Bardoxolone Methyl

For research use only.

Catalog No.S8078 Synonyms: RTA 402, TP-155, NSC 713200, CDDO Methyl Ester, CDDO-Me

17 publications

Bardoxolone Methyl Chemical Structure

CAS No. 218600-53-4

Bardoxolone Methyl (RTA 402, TP-155, NSC 713200, CDDO Methyl Ester, CDDO-Me) is an IKK inhibitor, showing potent proapoptotic and anti-inflammatory activities; Also a potent Nrf2 activator and nuclear factor-κB (NF-κB) inhibitor. Bardoxolone Methyl abrogates ferroptosis. Bardoxolone methyl induces apoptosis and autophagy in cancer cells.

Size Price Stock Quantity  
USD 97 In stock
USD 570 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Selleck's Bardoxolone Methyl has been cited by 17 publications

3 Customer Reviews

  • Renal Nrf2 activity was shown in RTA402-treated acFSGS (RTA402 + acFSGS) mice as early as day 7 (RTA402 + acFSGS) and persisted to day 28, compared to vehicle + acFSGS mice. Kidney in situ ROS production demonstrated by DHE detection.

    Free Radic Biol Med, 2014, 73:260-9 . Bardoxolone Methyl purchased from Selleck.

  • KG-1a cells were treated with Bar (0.5 µM) or a vehicle for 48 h and Annexin V/PI staining was detected after 48 h by flow cytometry.

    Oncol Rep, 2017, 38(3):1517-1524. Bardoxolone Methyl purchased from Selleck.

  • Cells were exposed to increasing concentrations of Bardoxolone methyl (BM; 0–1000 nM) and AR protein levels were measured. Top panels show representative immunoblots depicting AR-FL, AR-V7 and GAPDH levels. Bottom panels show fold change in AR proteins, normalized to GAPDH levels.

    Oncol Rep, 2017, 38(5):2774-2786. Bardoxolone Methyl purchased from Selleck.

Purity & Quality Control

Choose Selective IκB/IKK Inhibitors

Biological Activity

Description Bardoxolone Methyl (RTA 402, TP-155, NSC 713200, CDDO Methyl Ester, CDDO-Me) is an IKK inhibitor, showing potent proapoptotic and anti-inflammatory activities; Also a potent Nrf2 activator and nuclear factor-κB (NF-κB) inhibitor. Bardoxolone Methyl abrogates ferroptosis. Bardoxolone methyl induces apoptosis and autophagy in cancer cells.
Features The only IKKβ inhibitor in clinical use for solid tumors, type 2 diabetes, and chronic kidney disease. An orally-available antioxidant inflammation modulator.
IKK [3]
(Cell-free assay)
Ferroptosis [7]
Nrf2 [6]
NF-κB [6]
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MCF-7 cells MUDQdo9tcW[ncnH0bY9vKGG|c3H5 MUPJcohq[mm2b4L5JINwdmOnboTyZZRqd25iYXfhbY5{fCCycn;sbYZmemG2aX;uJI9nKE2FRj23JEhGWiCSb4PpeIl3\SliYoLlZZN1KGOjbnPldkBk\WyuczygTWM2OD1yLkC1JO69VQ>? M1voOFE2OzZ7M{m2
human CCD-841-CoN cells M4XHXnBzd2yrZnXyZZRqd25iYYPzZZk> MVO3NkBp M1H0dWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQ1PEMVg1OS2Fb16gZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iClZXzsJJBzd2yrZnXyZZRqd25iYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0xNjNzNjFOwG0> NUPqU5NROjV4N{WxOFQ>
human HCT8 cells M2DxNnBzd2yrZnXyZZRqd25iYYPzZZk> Mmr3O|IhcA>? MXHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiFVEigZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iClZXzsJJBzd2yrZnXyZZRqd25iYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0xNjN7OTFOwG0> NVWyfnRWOjV4N{WxOFQ>
human HepG2 cells MXLDfZRwfG:6aXRCpIF{e2G7 M3qwVFQ5KGh? M2ixfWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhmeEd{IHPlcIx{KGGodHXyJFQ5KGi{czDifUBOXFRiYYPzZZnwxIxiSVO1NF01Njl7IN88US=> M2DZW|I1Pjh3NUS1
mouse B16F10 cells NUWxUIo{S3m2b4TvfIlkyqCjc4PhfS=> NVKzXVBqPDhiaB?= NITqdmpEgXSxdH;4bYNqfHliYXfhbY5{fCCvb4Xz[UBDOT[IMUCgZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF02Njh3IN88US=> NFr2[GYzPDZ6NUW0OS=>
C57BL/6 mouse BMDM cells NH\2XItEgXSxdH;4bYPDqGG|c3H5 MoSyNlQhcA>? MoO3R5l1d3SxeHnjbZR6KGGpYXnud5QhSzV5QlyvOkBud3W|ZTDCUWROKGOnbHzzJIF{e2W|c3XkJIF{KEyGSDDy[Yxm[XOnIHHmeIVzKDJ2IHjydy=> NWfERnh4OjJ3M{O3PVA>
human HCT8 cells M1noXWZ2dmO2aX;uJIF{e2G7 NHzaW|cyKM7:TR?= M2HHc|I1KGh? NYnaeWdwUW6qaXLpeIlwdiCxZjDFVmsheHKxdHXpckBxcG:|cHjvdplt[XSrb36gbY4hcHWvYX6gTGNVQCClZXzsd{BifCBzIIXNJIlv[3WkYYTl[EBnd3JiMkSgbJJ{KGK7IGfld5Rmem5iYnzveJRqdmdibXX0bI9l NX[1VlAxOjV4N{WxOFQ>
mouse PANC1343 cells M37ZbHBzd2yrZnXyZZRqd25iYYPzZZk> NXjEUnM3OzByIITvJFExODBibl2= NX2yc3ZjPzJiaB?= MoPiRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDtc5V{\SCSQV7DNVM1OyClZXzsd{BifCB|MECgeI8hOTByMDDuUUBi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5 NVfNRW02OjR|OEi4NFY>
mouse RAW264.7 cells MmP4SpVv[3Srb36gZZN{[Xl? Mn33NVAxKG6P MWGxPEBp NVf1[4Z3SW62aX;4bYRidnRiYXP0bZZqfHliaX6gcY92e2ViUlHXNlY1NjdiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kB1SkiSLXnu[JVk\WRiUl;TJJBzd2S3Y4Tpc44h[XRiMUCwJI5OKHC{ZYTy[YF1\WRiZn;yJFE5KGi{czDi[YZwemViY3jhcIxmdmenIH3lZZN2emWmIHHmeIVzKDF3IH3pcpMh[nliSELER2ZCNWKjc3XkJIZtd3diY4n0c41mfHK7 NVTk[XZUOjR|OEi4NFY>
mouse PANC1343 cells MXnQdo9tcW[ncnH0bY9vKGG|c3H5 M2La[|MxOCC2bzCxNFAxKG6P NGHNOHk4OiCq NXfHUphoSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBud3W|ZTDQRW5EOTN2MzDj[YxteyCjdDCzNFAhfG9iMUCwNEBvVSCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6 NXT0eJBTOjR|OEi4NFY>

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Western blot
p-IκBα / IκBα ; 

PubMed: 25897966     

HeLa cells were pre-treated with RTA 408 or bardoxolone methyl for 6 hours at the indicated concentrations followed by a five-minute treatment with TNFα. Protein levels of phospho-IκBα and total IκBα were evaluated by western blot. Actin was used as loading control. Data are representative of four experiments.

Bcl-xl / Bcl-2 / Bax / Cleaved caspase / Cytochrome C / PARP / Cleaved PARP ; 

PubMed: 25733817     

Representative blots of respective proteins measured to show the effect of CDDO-Me treatment on the expression levels of Bcl-xl, Bcl-2, Bax, PUMA, cytochrome c, cleaved caspase-3 (active), cleaved caspase-9 (active), PARP, and cleaved PARP in Ec109 and KYSE70 cells determined using Western blotting analysis. 

p-PI3K / PI3K / p-AMPK / AMPK / p-p38 MAPK / p38 MAPK / p-AKT / AKT / p-mTOR / mTOR; 

PubMed: 25733817     

Effects of CDDO-Me treatment on the expression levels of p-PI3K at Tyr458, PI3K, p-AMPK at Thr172, AMPK, p-p38 at Thr180, p38, p-Akt at Ser473, Akt, p-mTOR at Ser2448, mTOR, PTEN, beclin 1, LC3-I, and LC3-II in Ec109 and KYSE70 cells. Cellular lysates were analyzed by immunoblotting with respective first antibody followed by the second antibody. 


PubMed: 22177954     

LNCaP and PC-3 cells were treated with CDDO-Me (0.3-5 µM) for 20 h and cell lysates were analyzed for PTEN, PP2A and PHLPP1 by immunoblotting. 

25897966 25733817 22177954

PubMed: 26053096     

MDA-MB 435 cells were treated with or without 1.5 μM CDDO-Me for indicated time points. Immunocytochemistry using anti-PDI (red) and anti-SDHA (green) antibodies was performed and the representative fluorescence and phase contrast microscopic images of cells are shown. Scale bar: 20 μm.

c-PARP / Cytochrome C / COX IV; 

PubMed: 26053096     

E, F. MDA-MB 435 cells were untreated or treated with 1.5 μM CDDO-Me for 24 h. Immunocytochemistry of the cleaved PARP and staining with DAPI were performed (E). Immunocytochemistry of the cytochrome c (Cyt.c) and the subunit I of cytochrome c oxidase (COX IV) was performed (F) Representative fluorescence microscopic images of cells are shown. Scale bars: 50 μm.

Growth inhibition assay
Cell viability ; 

PubMed: 25733817     

(A) The chemical structure of CDDO-Me and (B) effects of CDDO-Me on the proliferation of Ec109, KYSE70, and Het-1A cells determined by the MTT assay. Notes: Cells were treated with CDDO-Me at 0.01, 0.05, 0.25, 1.0, and 5.0 μM for 24 or 48 hours. Data are the mean ± SD of at least four independent experiments.

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]


Kinase Assay:


- Collapse

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 Research:


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

    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.

    (Only for Reference)
Animal Research:


- Collapse
  • Animal Models: Female A/J mice are injected i.p. with vinyl carbamate.
  • Dosages: ~60 mg/kg
  • Administration: Oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 21 mg/mL (41.52 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
4%DMSO+30% PEG300+5% Tween+61%ddH2O
For best results, use promptly after mixing.

* 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 Information

Molecular Weight 505.69


CAS No. 218600-53-4
Storage powder
in solvent
Synonyms RTA 402, TP-155, NSC 713200, CDDO Methyl Ester, CDDO-Me
Smiles CC1(CCC2(CCC3(C(C2C1)C(=O)C=C4C3(CCC5C4(C=C(C(=O)C5(C)C)C#N)C)C)C)C(=O)OC)C

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02316821 Completed Drug: RTA 402|Drug: Placebo Chronic Kidney Disease|Type 2 Diabetes Kyowa Kirin Co. Ltd. December 2014 Phase 2
NCT01598363 Completed Drug: Digoxin|Drug: Rosuvastatin Healthy Volunteers Reata Pharmaceuticals Inc. June 2012 Phase 1
NCT01551446 Withdrawn Drug: Bardoxolone Methyl Renal Insufficiency Chronic|Diabetes Mellitus Type 2 Reata Pharmaceuticals Inc. April 2012 Phase 1
NCT01503866 Completed Drug: bardoxolone methyl Healthy Reata Pharmaceuticals Inc. December 2011 Phase 1
NCT01461161 Completed Drug: bardoxolone methyl Healthy Volunteers Reata Pharmaceuticals Inc. October 2011 Phase 1

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.

Handling Instructions

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

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

  • * Indicates a Required Field

IκB/IKK Signaling Pathway Map

Related IκB/IKK Products

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