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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Cited by 3 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

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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.
Targets
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 M3X5SnBzd2yrZnXyZZRqd25iYYPzZZk> NILYNHhKdmirYnn0c5J6KGOxbnPlcpRz[XSrb36gZYdicW6|dDDwdo9tcW[ncnH0bY9vKG:oIF3DSk04KCiHUjDQc5NqfGm4ZTmgZpJm[XO2IHPhcoNmeiClZXzsd{whUUN3ME2wMlA2KM7:TR?= Ml6xNVU{Pjl|OU[=
human CCD-841-CoN cells M336XHBzd2yrZnXyZZRqd25iYYPzZZk> MlXXO|IhcA>? M2\2emFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQ1PEMVg1OS2Fb16gZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iClZXzsJJBzd2yrZnXyZZRqd25iYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0xNjNzNjFOwG0> MnTGNlU3PzVzNES=
human HCT8 cells M{HCZXBzd2yrZnXyZZRqd25iYYPzZZk> M2P5O|czKGh? NX2yVIpJSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIR3Q5KGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gZ4VtdCCycn;sbYZmemG2aX;uJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;MD6zPVkh|ryP NXHZOHhxOjV4N{WxOFQ>
human HepG2 cells NG\mXYxEgXSxdH;4bYPDqGG|c3H5 M4Ht[|Q5KGh? NEflXY5EgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJ\XCJMjDj[YxteyCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F697zOIFnDOVA:PC57OTFOwG0> MVuyOFY5PTV2NR?=
mouse B16F10 cells NGLNPHBEgXSxdH;4bYPDqGG|c3H5 NHnlRpo1QCCq MW\DfZRwfG:6aXPpeJkh[WejaX7zeEBud3W|ZTDCNVZHOTBiY3XscJMh[W[2ZYKgOFghcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME21Mlg2KM7:TR?= MnHBNlQ3QDV3NEW=
C57BL/6 mouse BMDM cells NGXLdFhEgXSxdH;4bYPDqGG|c3H5 MlLPNlQhcA>? NYnYephzS3m2b4TvfIlkcXS7IHHnZYlve3RiQ{W3RmwwPiCvb4Xz[UBDVUSPIHPlcIx{KGG|c3Xzd4VlKGG|IFzETEBz\WynYYPlJIFnfGW{IEK0JIhzew>? NVXG[nVIOjJ3M{O3PVA>
human HCT8 cells NV:1[3lwTnWwY4Tpc44h[XO|YYm= M3nFfFEh|ryP MknZNlQhcA>? NEnOdJpKdmirYnn0bY9vKG:oIFXST{Bxem:2ZXnuJJBpd3OyaH;yfYxifGmxbjDpckBpfW2jbjDIR3Q5KGOnbHzzJIF1KDFidV2gbY5kfWKjdHXkJIZweiB{NDDodpMh[nliV3XzeIVzdiCkbH;0eIlv\yCvZYToc4Q> M37Z[lI2Pjd3MUS0
mouse PANC1343 cells MkPuVJJwdGmoZYLheIlwdiCjc4PhfS=> MXOzNFAhfG9iMUCwNEBvVQ>? M1jkfFczKGh? MVTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IH3veZNmKFCDTlOxN|Q{KGOnbHzzJIF1KDNyMDD0c{AyODByIH7NJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYm= NWC4ZldiOjR|OEi4NFY>
mouse RAW264.7 cells NXm1ZodzTnWwY4Tpc44h[XO|YYm= MYqxNFAhdk1? MmrLNVghcA>? MVjBcpRqd3irZHHueEBi[3Srdnn0fUBqdiCvb4Xz[UBTSVd{NkSuO{Bk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIITCTHAucW6mdXPl[EBTV1NicILv[JVkfGmxbjDheEAyODBibl2gdJJmfHKnYYTl[EBnd3JiMUigbJJ{KGKnZn;y[UBkcGGubHXu[4UhdWWjc4Xy[YQh[W[2ZYKgNVUhdWmwczDifUBJOkSFRlGtZoF{\WRiZnzve{BkgXSxbXX0dpk> MUOyOFM5QDhyNh?=
mouse PANC1343 cells NW\BNJFrWHKxbHnm[ZJifGmxbjDhd5NigQ>? NVrGWIhVOzByIITvJFExODBibl2= NIX3[5E4OiCq NIXxeVJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JI1wfXOnIGDBUmMyOzR|IHPlcIx{KGG2IEOwNEB1dyBzMECwJI5OKGGodHXyJFczKGi{czDifUBOXFRiYYPzZZk> NXTkd4V[OjR|OEi4NFY>

... 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]

Protocol

Kinase Assay:

[3]

+ Expand

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:

[2]

+ Expand
  • 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:

[4]

+ Expand
  • 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.
5mg/mL

* 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
Formula

C32H43NO4

CAS No. 218600-53-4
Storage powder
in solvent
Synonyms RTA 402, TP-155, NSC 713200, CDDO Methyl Ester

Bio Calculators

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

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

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

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The Serial Dilution Calculator Equation

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03749447 Not yet recruiting Chronic Kidney Diseases|Alport Syndrome Reata Pharmaceuticals Inc. February 2019 Phase 3
NCT03749447 Not yet recruiting Chronic Kidney Diseases|Alport Syndrome Reata Pharmaceuticals Inc. February 2019 Phase 3
NCT03550443 Recruiting Diabetic Kidney Disease Kyowa Hakko Kirin Co. Ltd May 30 2018 Phase 3
NCT03550443 Recruiting Diabetic Kidney Disease Kyowa Hakko Kirin Co. Ltd May 30 2018 Phase 3
NCT03366337 Active not recruiting IgA Nephropathy|CKD Associated With Type 1 Diabetes|Focal Segmental Glomerulosclerosis|Autosomal Dominant Polycystic Kidney Reata Pharmaceuticals Inc. December 26 2017 Phase 2
NCT03366337 Active not recruiting IgA Nephropathy|CKD Associated With Type 1 Diabetes|Focal Segmental Glomerulosclerosis|Autosomal Dominant Polycystic Kidney Reata Pharmaceuticals Inc. December 26 2017 Phase 2

Tech Support

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID