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Bardoxolone Methyl (TP-155) 是一种合成的三萜类化合物,作为 Nrf2通路的激活剂和 NF-κB 途径的抑制剂,具有潜在的抗肿瘤和抗炎活性。
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Bardoxolone Methyl (TP-155) 是一种合成的三萜类化合物,作为 Nrf2通路的激活剂和 NF-κB 途径的抑制剂,具有潜在的抗肿瘤和抗炎活性。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
5 mg | ¥ 257 | 现货 | |
10 mg | ¥ 398 | 现货 | |
25 mg | ¥ 637 | 现货 | |
50 mg | ¥ 828 | 现货 | |
100 mg | ¥ 1,230 | 现货 | |
200 mg | ¥ 1,980 | 现货 | |
500 mg | ¥ 3,370 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 452 | 现货 |
产品描述 | 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. |
体外活性 | 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] |
体内活性 | 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] |
激酶实验 | 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. |
细胞实验 | 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) |
别名 | 甲基巴多索隆, TP-155, RTA 402, NSC 713200, CDDO Methyl ester |
分子量 | 505.69 |
分子式 | C32H43NO4 |
CAS No. | 218600-53-4 |
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 |
密度 | 1.15g/cm3 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||
溶解度信息 | H2O: < 1 mg/mL (insoluble or slightly soluble) DMSO: 18.33 mg/mL (36.25 mM) Ethanol: < 1 mg/mL (insoluble or slightly soluble) | |||||||||||||||||||||||||
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