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Bardoxolone is an IKK inhibitor, showing potent proapoptotic and anti-inflammatory activities; Also a potent Nrf2 activator and nuclear factor-κB (NF-κB) inhibitor.
In vitro: Bardoxolone 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 (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.
| Cell Experiment | |
|---|---|
| Cell lines | HL-60, KG-1, and NB4 cells |
| Preparation method | Leukemic cell lines are cultured at a density of 3.0 × 10^5 cells/mL, and AML mononuclear cells are cultured at 5 × 10^5 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. |
| Concentrations | ~5 μM |
| Incubation time | 72 hours |
| Animal Experiment | |
|---|---|
| Animal models | Female A/J mice are injected i.p. with vinyl carbamate. |
| Formulation | DMSO |
| Dosages | ~60 mg/kg |
| Administration | Oral gavage |
| Molecular Weight | 491.66 |
| Formula | C31H41NO4 |
| CAS Number | 218600-44-3 |
| Solubility (25°C) | 21 mg/mL in DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related IκB/IKK Products |
|---|
| ACHP
ACHP is a selective and orally active IκB kinase inhibitor with IC50 values of 8.5 nM and 250 nM for IKKβ and IKKα, respectively. |
| BMS-066
BMS-066 is an IKKβ/Tyk2 pseudokinase inhibitor, with IC50s of 9 nM and 72 nM, respectively. |
| Ainsliadimer A
Ainsliadimer A is a novel guaiacolide sesquiterpene dimer isolated from Ainsliaea macrocephala.Ainsliadimer A can block the NF-κB signaling pathway by binding to IKK α/β, and possesses anti-tumor and anti-inflammatory activities.Meanwhile, Ainsliadimer A can also Ainsliadimer A can also directly target peroxidase 1 and 2 (PRDX1 and PRDX2) and significantly inhibit their enzymatic activities. In addition, Ainsliadimer A can cause mitochondrial dysfunction by altering the permeability of mitochondrial membrane potential, inhibiting mitochondrial respiration and ATP production, inhibiting cell proliferation, promoting cell cycle arrest in G2/M phase, and inducing apoptosis. |
| IKK2-IN-4
IKK2-IN-4 is a potent IKK-2 inhibitor, with an IC50 of 25 nM. |
| MRT67307 dihydrochloride
MRT67307 dihydrochloride is a dual inhibitor of the IKKε and TBK-1 with IC50s of 160 and 19 nM, respectively. |
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