Bardoxolone Methyl
Catalog No.S8078 Synonyms: RTA 402, TP-155, NSC 713200, CDDO Methyl Ester
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.
Cited by 3 Publications
3 Customer Reviews
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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.
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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 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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| Features | The only IKKβ inhibitor in clinical use for solid tumors, type 2 diabetes, and chronic kidney disease. An orally-available antioxidant inflammation modulator. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| 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] |
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| Cell Data |
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| 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: |
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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. |
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| Animal Research: |
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Solubility (25°C)
| In vitro | DMSO | 21 mg/mL (41.52 mM) |
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| 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 |
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| 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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Molarity Calculator
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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