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Bardoxolone Methyl

Catalog No. T6165   CAS 218600-53-4
Synonyms: RTA 402, CDDO Methyl ester, TP-155, NSC 713200

Bardoxolone Methyl (TP-155) is a synthetic triterpenoid that acts as an activator of the Nrf2 pathway and an inhibitor of the NF-κB pathway with potential anti-tumor and anti-inflammatory activities.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
Bardoxolone Methyl Chemical Structure
Bardoxolone Methyl, CAS 218600-53-4
Pack Size Availability Price/USD Quantity
10 mg In stock $ 39.00
25 mg In stock $ 59.00
50 mg In stock $ 80.00
100 mg In stock $ 122.00
200 mg In stock $ 197.00
500 mg In stock $ 447.00
1 mL * 10 mM (in DMSO) In stock $ 43.00
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Purity: 99.09%
Purity: 98.94%
Purity: 97.81%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Bardoxolone Methyl (TP-155) is a synthetic triterpenoid that acts as an activator of the Nrf2 pathway and an inhibitor of the NF-κB pathway with potential anti-tumor and anti-inflammatory activities.
In vitro Bardoxolone Methyl exhibits potent inhibitory activities against production of nitric oxide induced by interferon-? 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]
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]
Kinase Assay 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 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)
Synonyms RTA 402, CDDO Methyl ester, TP-155, NSC 713200
Molecular Weight 505.69
Formula C32H43NO4
CAS No. 218600-53-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 20 mg/mL (39.5 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

TargetMolReferences and Literature

1. Honda T, et al. J Med Chem. 2000, 43(22), 4233-4246. 2. Konopleva M, et al. Blood. 2002, 99(1), 326-335. 3. Shishodia S, et al. Clin Cancer Res. 2006, 12(6), 1828-1838. 4. Liby K, et al. Cancer Res. 2007, 67(6), 2414-2419. 5. Auletta JJ, et al. J Interferon Cytokine Res. 2010, 30(7), 497-508.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Active Compound Library Anti-Cancer Drug Library Anti-Cancer Approved Drug Library Anti-Cancer Clinical Compound Library Pediatric Drug Library FDA-Approved Kinase Inhibitor Library Pyroptosis Compound Library Immunology/Inflammation Compound Library Anti-Cancer Compound Library Apoptosis Compound Library

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Keywords

Bardoxolone Methyl 218600-53-4 Apoptosis Autophagy Immunology/Inflammation NF-Κb Nrf2 Ferroptosis IκB/IKK RTA 402 CDDO Methyl ester TP155 inhibit Keap1-Nrf2 Inhibitor NSC713200 RTA-402 RTA402 TP-155 NSC 713200 TP 155 NSC-713200 inhibitor

 

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