Bardoxolone Methyl

製品コードS8078 バッチS807802

印刷

化学情報

Chemical Structure Synonyms RTA 402, TP-155, NSC 713200, CDDO Methyl Ester, CDDO-Me Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C32H43NO4
分子量 505.69 CAS No. 218600-53-4
Solubility (25°C)* 体外 DMSO 21 mg/mL (41.52 mM)
Water Insoluble
Ethanol Insoluble
* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Bardoxolone Methyl (RTA 402, TP-155, NSC 713200, CDDO Methyl Ester, CDDO-Me) is an IKK inhibitor, showing potent proapoptotic and anti-inflammatory activities; Also a potent Nrf2 activator and nuclear factor-κB (NF-κB) inhibitor. Bardoxolone Methyl abrogates ferroptosis. Bardoxolone methyl induces apoptosis and autophagy in cancer cells.
in vitro

Bardoxolone Methyl exhibits potent inhibitory activities against production of nitric oxide induced by interferon-Ƴ 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]
特徴 The only IKKβ inhibitor in clinical use for solid tumors, type 2 diabetes, and chronic kidney disease. An orally-available antioxidant inflammation modulator.

プロトコル(参考用のみ)

キナーゼアッセイ 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.
細胞アッセイ 細胞株 HL-60, KG-1, and NB4 cells
濃度 ~5 μM
反応時間 72 hours
実験の流れ

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.
動物実験 動物モデル Female A/J mice are injected i.p. with vinyl carbamate.
投薬量 ~60 mg/kg
投与方法 Oral gavage

カスタマーフィードバック

Data from [Data independently produced by , , Free Radic Biol Med, 2014, 73:260-9 ]

Data from [Data independently produced by , , Oncol Rep, 2017, 38(3):1517-1524]

Data from [Data independently produced by , , Oncol Rep, 2017, 38(5):2774-2786]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

USP25 regulates KEAP1-NRF2 anti-oxidation axis and its inactivation protects acetaminophen-induced liver injury in male mice [ Nat Commun, 2023, 14(1):3648] PubMed: 37339955
Association of NRF2 with HIF-2α-induced cancer stem cell phenotypes in chronic hypoxic condition [ Redox Biol, 2023, 60:102632] PubMed: 36791645
Human iPSC-derived renal collecting duct organoid model cystogenesis in ADPKD [ Cell Rep, 2023, 42(12):113431] PubMed: 38039961
Transcriptional landscape of mitochondrial electron transport chain inhibition in renal cells [ Cell Biol Toxicol, 2023, 10.1007/s10565-023-09816-7] PubMed: 37353587
Synthetic oleanane triterpenoids suppress MYB oncogene activity and sensitize T-cell acute lymphoblastic leukemia cells to chemotherapy [ Front Oncol, 2023, 13:1126354] PubMed: 37077825
2,3,5,4'-Tetrahydroxystilbene -TG1), a Novel Compound Derived from 2,3,5,4'-Tetrahydroxystilbene-2-O-β-D-glucoside -THSG), Inhibits Colorectal Cancer Progression by Inducing Ferroptosis, Apoptosis, and Autophagy [ Biomedicines, 2023, 11(7)1798] PubMed: 37509438
Snail acetylation by autophagy-derived acetyl-coenzyme A promotes invasion and metastasis of KRAS-LKB1 co-mutated lung cancer cells [ Cancer Commun (Lond), 2022, 42(8):716-749] PubMed: 35838183
Snail acetylation by autophagy-derived acetyl-coenzyme A promotes invasion and metastasis of KRAS-LKB1 co-mutated lung cancer cells [ Cancer Commun (Lond), 2022, 10.1002/cac2.12332] PubMed: 35838183
NRF2 is a critical regulator and therapeutic target of metal implant particle-incurred bone damage [ Biomaterials, 2022, 288:121742] PubMed: 36030105
Z-REX uncovers a bifurcation in function of Keap1 paralogs [ Elife, 2022, 11e83373] PubMed: 36300632

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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