Bardoxolone Methyl

SKU: orb1301019

Description

Bardoxolone Methyl (TP-155) is a synthetic triterpenoid that activates the Nrf2 antioxidant pathway while inhibiting the pro-inflammatory NF-κB pathway. It has demonstrated anti-inflammatory and potential anti-tumor activity in various in vitro and in vivo research models, including studies on kidney disease and cancer.

Research Area

Cell Biology, Immunology & Inflammation, Infectious Disease & Virology, Signal Transduction

Key Properties

• CAS Number: 218600-53-4
• MW: 505.69
• Purity: 98.94%
• Formula: C₃₂H₄₃NO₄
• SMILES: [H][C@@]12CC(C)(C)CC[C@@]1(CC[C@]1(C)C2C(=O)C=C2[C@@]1(C)CC[C@@]1([H])C(C)(C)C(=O)C(=C[C@]21C)C#N)C(=O)OC
• Target: IκB/IKK,Virus Protease,Ferroptosis,Apoptosis,Autophagy,Nrf2,SARS-CoV
• Solubility: DMSO:40.83 mg/mL (80.74 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.95 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• 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.
• 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. 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.
• 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)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Inhibitor, Ferroptosis, IkB, IkB/IKK, IKK, inhibit, IκB, Keap1-Nrf2, NSC713200, NSC-713200, NSC 713200, CDDO Methyl ester, Autophagy, Apoptosis, Bardoxolone Methyl, TP 155, TP155, TP-155, RTA 402, RTA402, RTA-402

Compound Identifiers

PubChem CID

70700216