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. Phase 3.
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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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|Description||Bardoxolone Methyl is an IKK inhibitor, showing potent proapoptotic and anti-inflammatory activities. Phase 3.|
|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)|
|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|
|NCT02657356||Not yet 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 Company, Limited||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|
|NCT01576887||Withdrawn||End-Stage Renal Disease|Type 2 Diabetes Mellitus||Reata Pharmaceuticals, Inc.||July 2012||Phase 2|
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