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 7 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.

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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 MkfDVJJwdGmoZYLheIlwdiCjc4PhfS=> NXfEPVhIUW6qaXLpeI9zgSClb37j[Y51emG2aX;uJIFo[Wmwc4SgdJJwdGmoZYLheIlwdiCxZjDNR2YuPyBqRWKgVI9{cXSrdnWpJIJz\WG|dDDjZY5k\XJiY3XscJMtKEmFNUC9NE4xPSEQvF2= MWixOVM3QTN7Nh?=
human CCD-841-CoN cells MlqzVJJwdGmoZYLheIlwdiCjc4PhfS=> NFPLUpU4OiCq MWjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEOFRD24OFEuS2:QIHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4Yh[2WubDDwdo9tcW[ncnH0bY9vKGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUC9NE4{OTZizszN M3;YOlI2Pjd3MUS0
human HCT8 cells NFjpO2tRem:uaX\ldoF1cW:wIHHzd4F6 MoW1O|IhcA>? MnO3RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKQ2S4JINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiY3XscEBxem:uaX\ldoF1cW:wIHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:OC5|OUmg{txO M4fJTVI2Pjd3MUS0
human HepG2 cells MUDDfZRwfG:6aXRCpIF{e2G7 MkjHOFghcA>? M4Tx[2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhmeEd{IHPlcIx{KGGodHXyJFQ5KGi{czDifUBOXFRiYYPzZZnwxIxiSVO1NF01Njl7IN88US=> NX;0XINzOjR4OEW1OFU>
mouse B16F10 cells M2CySmN6fG:2b4jpZ:Kh[XO|YYm= NEXqbII1QCCq MY\DfZRwfG:6aXPpeJkh[WejaX7zeEBud3W|ZTDCNVZHOTBiY3XscJMh[W[2ZYKgOFghcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME21Mlg2KM7:TR?= MmfXNlQ3QDV3NEW=
C57BL/6 mouse BMDM cells MmHkR5l1d3SxeHnjxsBie3OjeR?= MYGyOEBp M3\O[GN6fG:2b4jpZ4l1gSCjZ3HpcpN1KEN3N1LMM|YhdW:3c3WgRm1FVSClZXzsd{Bie3Onc4Pl[EBieyCORFigdoVt\WG|ZTDh[pRmeiB{NDDodpM> NV\HZ3VWOjJ3M{O3PVA>
human HCT8 cells NGfHOodHfW6ldHnvckBie3OjeR?= NGj2U4syKM7:TR?= Mn;INlQhcA>? M2LHNWlvcGmkaYTpc44hd2ZiRWLLJJBzd3SnaX6gdIhwe3Cqb4L5cIF1cW:wIHnuJIh2dWGwIFjDWFgh[2WubIOgZZQhOSC3TTDpcoN2[mG2ZXSg[o9zKDJ2IHjyd{BjgSCZZYP0[ZJvKGKub4T0bY5oKG2ndHjv[C=> Mm\yNlU3PzVzNES=
mouse PANC1343 cells NH\tO21Rem:uaX\ldoF1cW:wIHHzd4F6 MV:zNFAhfG9iMUCwNEBvVQ>? MoTpO|IhcA>? NWL1Zmk2SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBud3W|ZTDQRW5EOTN2MzDj[YxteyCjdDCzNFAhfG9iMUCwNEBvVSCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6 NHnj[YozPDN6OEiwOi=>
mouse RAW264.7 cells MXjGeY5kfGmxbjDhd5NigQ>? NYKz[4tqOTByIH7N NYfB[G9pOThiaB?= MULBcpRqd3irZHHueEBi[3Srdnn0fUBqdiCvb4Xz[UBTSVd{NkSuO{Bk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIITCTHAucW6mdXPl[EBTV1NicILv[JVkfGmxbjDheEAyODBibl2gdJJmfHKnYYTl[EBnd3JiMUigbJJ{KGKnZn;y[UBkcGGubHXu[4UhdWWjc4Xy[YQh[W[2ZYKgNVUhdWmwczDifUBJOkSFRlGtZoF{\WRiZnzve{BkgXSxbXX0dpk> NYrEdY42OjR|OEi4NFY>
mouse PANC1343 cells M1fFOXBzd2yrZnXyZZRqd25iYYPzZZk> NFrRcGU{ODBidH:gNVAxOCCwTR?= MWm3NkBp NF75[opCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JI1wfXOnIGDBUmMyOzR|IHPlcIx{KGG2IEOwNEB1dyBzMECwJI5OKGGodHXyJFczKGi{czDifUBOXFRiYYPzZZk> MXmyOFM5QDhyNh?=

... Click to View More Cell Line Experimental Data
Assay
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. 

PTEN / PP2A / PHLPP1 ; 

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
Immunofluorescence
PDI / SDHA ; 

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.

26053096
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.

25733817
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]
- 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:

[2]
- 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:

[4]
- Collapse
  • 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

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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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID