Bardoxolone Methyl

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

Bardoxolone Methyl Chemical Structure

Molecular Weight(MW): 505.69

Bardoxolone Methyl is an IKK inhibitor, showing potent proapoptotic and anti-inflammatory activities; Also a potent Nrf2 activator and nuclear factor-κB (NF-κB) inhibitor.

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1 Customer Review

  • 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.

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Biological Activity

Description Bardoxolone Methyl is an IKK inhibitor, showing potent proapoptotic and anti-inflammatory activities; Also a potent Nrf2 activator and nuclear factor-κB (NF-κB) inhibitor.
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)
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 NIDMXFFRem:uaX\ldoF1cW:wIHHzd4F6 M3zBNWlvcGmkaYTvdpkh[2:wY3XueJJifGmxbjDh[4FqdnO2IIDyc4xq\mW{YYTpc44hd2ZiTVPGMVchMEWUIGDvd4l1cX[nKTDidoVie3RiY3HuZ4VzKGOnbHzzMEBKSzVyPUCuNFUh|ryP NGrvS48yPTN4OUO5Oi=>
human CCD-841-CoN cells NVv4OXI6WHKxbHnm[ZJifGmxbjDhd5NigQ>? NUDnWodwPzJiaB?= MULBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEOFRD24OFEuS2:QIHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4Yh[2WubDDwdo9tcW[ncnH0bY9vKGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUC9NE4{OTZizszN NF:wPHQzPTZ5NUG0OC=>
human HCT8 cells NHjOW5dRem:uaX\ldoF1cW:wIHHzd4F6 MlP4O|IhcA>? MmnURY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKQ2S4JINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiY3XscEBxem:uaX\ldoF1cW:wIHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:OC5|OUmg{txO M3PxWVI2Pjd3MUS0
human HepG2 cells MXrDfZRwfG:6aXRCpIF{e2G7 NFSyZ|k1QCCq M336cWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhmeEd{IHPlcIx{KGGodHXyJFQ5KGi{czDifUBOXFRiYYPzZZnwxIxiSVO1NF01Njl7IN88US=> MY[yOFY5PTV2NR?=
mouse B16F10 cells Ml7QR5l1d3SxeHnjxsBie3OjeR?= M3LLVlQ5KGh? M2\QUWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KG2xdYPlJGIyPkZzMDDj[YxteyCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVUvQDVizszN MXeyOFY5PTV2NR?=
C57BL/6 mouse BMDM cells M4PGbWN6fG:2b4jpZ:Kh[XO|YYm= NWnrdZNJOjRiaB?= NUjlVoZ4S3m2b4TvfIlkcXS7IHHnZYlve3RiQ{W3RmwwPiCvb4Xz[UBDVUSPIHPlcIx{KGG|c3Xzd4VlKGG|IFzETEBz\WynYYPlJIFnfGW{IEK0JIhzew>? NIjoSokzOjV|M{e5NC=>
human HCT8 cells NES5epRHfW6ldHnvckBie3OjeR?= NUTXOZROOSEQvF2= NXzaSlQ2OjRiaB?= NIiwWIxKdmirYnn0bY9vKG:oIFXST{Bxem:2ZXnuJJBpd3OyaH;yfYxifGmxbjDpckBpfW2jbjDIR3Q5KGOnbHzzJIF1KDFidV2gbY5kfWKjdHXkJIZweiB{NDDodpMh[nliV3XzeIVzdiCkbH;0eIlv\yCvZYToc4Q> M37H[FI2Pjd3MUS0
mouse PANC1343 cells NI\2eXJRem:uaX\ldoF1cW:wIHHzd4F6 NU[4WYN3OzByIITvJFExODBibl2= Mm\nO|IhcA>? MnzXRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDtc5V{\SCSQV7DNVM1OyClZXzsd{BifCB|MECgeI8hOTByMDDuUUBi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5 NYf6VFZUOjR|OEi4NFY>
mouse RAW264.7 cells M3;pWGZ2dmO2aX;uJIF{e2G7 NHizUVkyODBibl2= NXXNOW1iOThiaB?= MX\BcpRqd3irZHHueEBi[3Srdnn0fUBqdiCvb4Xz[UBTSVd{NkSuO{Bk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIITCTHAucW6mdXPl[EBTV1NicILv[JVkfGmxbjDheEAyODBibl2gdJJmfHKnYYTl[EBnd3JiMUigbJJ{KGKnZn;y[UBkcGGubHXu[4UhdWWjc4Xy[YQh[W[2ZYKgNVUhdWmwczDifUBJOkSFRlGtZoF{\WRiZnzve{BkgXSxbXX0dpk> MVuyOFM5QDhyNh?=
mouse PANC1343 cells M4nDXHBzd2yrZnXyZZRqd25iYYPzZZk> M3LyclMxOCC2bzCxNFAxKG6P MWO3NkBp Mn74RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDtc5V{\SCSQV7DNVM1OyClZXzsd{BifCB|MECgeI8hOTByMDDuUUBi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5 NHfsVFkzPDN6OEiwOi=>

... Click to View More Cell Line Experimental Data

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:


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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:


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  • 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:


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  • Animal Models: Female A/J mice are injected i.p. with vinyl carbamate.
  • Formulation: DMSO
  • 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% PEG 300+5% Tween+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

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03019185 Recruiting Alport Syndrome Reata Pharmaceuticals, Inc. February 2017 Phase 2|Phase 3
NCT02657356 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 Co., Ltd 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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID