名称 | Oltipraz |
描述 | Oltipraz (RP 35972) is a synthetic dithiolethione with potential chemopreventive and anti-angiogenic properties. Oltipraz induces phase II detoxification enzymes, such as glutathione S transferase (GST) and NAD(P)H: quinone oxidoreductase 1 (NQO1). The induction of detoxification enzymes enhances the detoxification of certain cancer-causing agents, thereby enhancing their elimination and preventing carcinogen-induced DNA damages. Although the exact mechanism through which the anti-angiogenesis effect remains to be fully elucidated, oltipraz maybe able to modulate the expression of a number of angiogenic factors, thereby blocking the sustained and focal neovascularization in multiple tumor cell types. |
激酶实验 | The Src and Abl kinase assays: The Src kinase activity is measured in an ELISA format. Src (3 units/reaction), reaction buffer (50 mM Tris-HCl pH 7.5, 10 mM MgCl2, 0.1 mM EGTA, 0.5 mM Na3VO4) and cdc2 substrate peptide are added to various concentration of Bosutinib and incubated at 30 °C for 10 minutes. The reaction is started by the addition of ATP to a final concentration of 100 μM, incubated at 30 °C for 1 hour and stopped by addition of EDTA. Instructions from the manufacturer are followed for subsequent steps. The Abl kinase assay is performed in a DELFIA solid phase europium-based detection assay format. Biotinylated peptide (2 μM) is bound to streptavidin-coated microtitration plates for 1.5 hours in 1 mg/mL ovalbumin in PBS. The plates are washed for 1 hour with PBS/0.1% Tween 80, followed by a PBS wash. The kinase reaction is incubated for 1 hour at 30°C. Abl kinase (10 units) is mixed with 50 mM Tris-HCl (pH 7.5), 10 mM MgCl2, 80 μM EGTA, 100 μM ATP, 0.5 mM Na3VO4, 1% DMSO, 1 mM HEPES (pH 7.0), 200 μg/mL ovalbumin and various concentration of Bosutinib. The reaction is stopped with EDTA at a final concentration of 50 mM. The reaction is monitored with Eu-labeled phosphotyrosine antibody and DELFIA enhancement solution. |
体外活性 | 作为一种化学保护剂,Oltipraz 能以 Nrf2 依赖性方式诱导第二阶段解毒酶的活性。[1] 在人类 HT29 结肠癌细胞中,奥替普拉唑通过显著加速 HIF-1α 蛋白的降解,抑制胰岛素、缺氧或 CoCl2 对 HIF-1α 的诱导。[2] |
体内活性 | Oltipraz(500 mg/kg,口服)可显著降低野生型小鼠胃肿瘤的复发率 55%,但对 nrf2 缺失型小鼠的肿瘤负荷没有影响。[1] 在移植了 HCT116 细胞的 BALB/c 裸鼠体内,Oltipraz(200 mg/kg,口服)通过抑制 HIF-1α 抑制肿瘤生长和血管生成。[2] 在以 CDAA 为食的大鼠中,Oltipraz 可减轻非酒精性脂肪性肝炎相关纤维化的进展。[3] |
存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | DMSO : 15 mg/mL (66.27 mM), Sonication is recommended.
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关键字 | Inhibitor | HIF/HIF Prolyl-Hydroxylase | Oltipraz | Keap1-Nrf2 | RP35972 | inhibit | HIFs | Human immunodeficiency virus | HIV | Hypoxia-inducible factors | NSC347901 | NSC-347901 | RP-35972 | HIF-PH |
相关产品 | Valproic Acid | Hydroxycitric acid tripotassium hydrate | Emtricitabine | Glucosamine | Lamivudine | 5-Fluorouracil | Curcumin | Decanedioic acid | Dextran sulfate sodium salt (MW 4500-5500) | Stavudine | Kaempferol | Dimethyl fumarate |
相关库 | 抗癌活性化合物库 | 经典已知活性库 | 已知活性化合物库 | 抗癌细胞代谢库 | 抗衰老化合物库 | 抗病毒库 | 神经退行性疾病化合物库 | 药物功能重定位化合物库 | 抗癌临床化合物库 | 抗癌药物库 |