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 MonjVJJwdGmoZYLheIlwdiCjc4PhfS=> NFLmZlFKdmirYnn0c5J6KGOxbnPlcpRz[XSrb36gZYdicW6|dDDwdo9tcW[ncnH0bY9vKG:oIF3DSk04KCiHUjDQc5NqfGm4ZTmgZpJm[XO2IHPhcoNmeiClZXzsd{whUUN3ME2wMlA2KM7:TR?= M{fJW|E2OzZ7M{m2
human CCD-841-CoN cells M1HoeXBzd2yrZnXyZZRqd25iYYPzZZk> MWG3NkBp MU\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEOFRD24OFEuS2:QIHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4Yh[2WubDDwdo9tcW[ncnH0bY9vKGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUC9NE4{OTZizszN NU[4fYU4OjV4N{WxOFQ>
human HCT8 cells NXW4PGw6WHKxbHnm[ZJifGmxbjDhd5NigQ>? NVHMRVdYPzJiaB?= M4PKdmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFPUPEBk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIHPlcIwheHKxbHnm[ZJifGmxbjDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTBwM{m5JO69VQ>? MX:yOVY4PTF2NB?=
human HepG2 cells NEH3blhEgXSxdH;4bYPDqGG|c3H5 NV7JeIFqPDhiaB?= MnTiR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTIVxTzJiY3XscJMh[W[2ZYKgOFghcHK|IHL5JG1VXCCjc4Phfg+9lCCLQ{WwQVQvQTlizszN M{jOTVI1Pjh3NUS1
mouse B16F10 cells NVTvUXBvS3m2b4TvfIlkyqCjc4PhfS=> NVLxfFdXPDhiaB?= NFfkVJFEgXSxdH;4bYNqfHliYXfhbY5{fCCvb4Xz[UBDOT[IMUCgZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF02Njh3IN88US=> NXrlOGdSOjR4OEW1OFU>
C57BL/6 mouse BMDM cells MVjDfZRwfG:6aXRCpIF{e2G7 M2DhWVI1KGh? M3LnTGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KEN3N1LMM|YhdW:3c3WgRm1FVSClZXzsd{Bie3Onc4Pl[EBieyCORFigdoVt\WG|ZTDh[pRmeiB{NDDodpM> M{ix[VIzPTN|N{mw
human HCT8 cells M{TJbWZ2dmO2aX;uJIF{e2G7 MX[xJO69VQ>? NIW5dJkzPCCq MmLhTY5pcWKrdHnvckBw\iCHUlugdJJwfGWrbjDwbI9{eGixconsZZRqd25iaX6gbJVu[W5iSFPUPEBk\WyuczDheEAyKHWPIHnuZ5Vj[XSnZDDmc5IhOjRiaILzJIJ6KFenc4Tldo4h[myxdITpcochdWW2aH;k MYeyOVY4PTF2NB?=
mouse PANC1343 cells M1XtfnBzd2yrZnXyZZRqd25iYYPzZZk> MVqzNFAhfG9iMUCwNEBvVQ>? MnTaO|IhcA>? NUXabXljSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBud3W|ZTDQRW5EOTN2MzDj[YxteyCjdDCzNFAhfG9iMUCwNEBvVSCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6 MX2yOFM5QDhyNh?=
mouse RAW264.7 cells M4\zZmZ2dmO2aX;uJIF{e2G7 Mni5NVAxKG6P NXPreXhOOThiaB?= MoGwRY51cW:6aXThcpQh[WO2aY\peJkhcW5ibX;1d4UhWkGZMk[0Mlch[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjD0RmhRNWmwZIXj[YQhWk:VIIDyc4R2[3Srb36gZZQhOTByIH7NJJBz\XS{ZXH0[YQh\m:{IEG4JIhzeyCkZX\vdoUh[2ijbHzlcodmKG2nYYP1doVlKGGodHXyJFE2KG2rboOgZpkhUDKGQ1\BMYJie2WmIH\sc5ch[3m2b33leJJ6 NXj2b2lnOjR|OEi4NFY>
mouse PANC1343 cells MWnQdo9tcW[ncnH0bY9vKGG|c3H5 NWOy[4J1OzByIITvJFExODBibl2= MWO3NkBp M17HXWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgcY92e2ViUFHOR|E{PDNiY3XscJMh[XRiM{CwJJRwKDFyMECgcm0h[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfS=> M2rYcVI1Ozh6OEC2

... 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
NCT02657356 Recruiting Connective Tissue Disease-Associated Pulmonary Arterial Hypertension Reata Pharmaceuticals Inc. October 4 2016 Phase 3
NCT03550443 Recruiting Diabetic Kidney Disease Kyowa Hakko Kirin Co. Ltd May 30 2018 Phase 3
NCT03366337 Recruiting IgA Nephropathy|CKD Associated With Type 1 Diabetes|Focal Segmental Glomerulosclerosis|Autosomal Dominant Polycystic Kidney Reata Pharmaceuticals Inc. December 26 2017 Phase 2
NCT02316821 Completed Chronic Kidney Disease|Type 2 Diabetes Kyowa Hakko Kirin Co. Ltd December 2014 Phase 2
NCT02036970 Completed Pulmonary Arterial Hypertension|Pulmonary Hypertension|Interstitial Lung Disease|Idiopathic Interstitial Pneumonia|Idiopathic Pulmonary Fibrosis|Sarcoidosis|Respiratory Bronchiolitis Associated Interstitial Lung Disease|Desquamative Interstitial Pneumonia|Cryptogenic Organizing Pneumonia|Acute Interstitial Pneumonitis|Idiopathic Lymphoid Interstitial Pneumonia|Idiopathic Pleuroparenchymal Fibroelastosis Reata Pharmaceuticals Inc. May 2014 Phase 2
NCT01655186 Withdrawn Renal Insufficiency Chronic|Diabetes Mellitus Type 2 Reata Pharmaceuticals Inc. September 2012 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID