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.
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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.
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Choose Selective IκB/IKK Inhibitors
|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.|
Bardoxolone Methyl exhibits potent inhibitory activities against production of nitric oxide induced by interferon-Ƴ in mouse macrophages with IC50 of 0.1 nM.  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.  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. 
|In vivo||Bardoxolone Methyl (60 mg/kg) reduces the number, size, and severity of lung tumors in vivo.  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. |
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.
-  Honda T, et al. J Med Chem. 2000, 43(22), 4233-4246.
-  Konopleva M, et al. Blood. 2002, 99(1), 326-335.
-  Shishodia S, et al. Clin Cancer Res. 2006, 12(6), 1828-1838.
|In vitro||DMSO||21 mg/mL (41.52 mM)|
|Water||slightly soluble or insoluble|
|Ethanol||slightly soluble or insoluble|
|In vivo||4% DMSO+30% PEG 300+5% Tween+ddH2O||5mg/mL|
* 1 mg/ml means slightly soluble or insoluble.
* 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.
|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|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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