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Product IntroductionBioactivity英文名: Oltipraz描述: Oltipraz (RP 35972) 是一种 Nrf2的强效激活剂。它时间依赖性地抑制 HIF-1α激活，IC50为 10 μM，浓度 ≥ 10
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Product Introduction
Bioactivity
英文名: Oltipraz
描述: Oltipraz (RP 35972) 是一种 Nrf2的强效激活剂。它时间依赖性地抑制 HIF-1α激活，IC50为 10 μM，浓度 ≥ 10 μM 时完全消除 HIF-1α诱导。
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
溶解度: DMSO : 15 mg/mL (66.27 mM)
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: PHD2-IN-1 | SYP-5 | AKBA | Oroxylin A | M1001 | Panaxadiol | HIF-2α-IN-9 | PHD-1-IN-1 | EHP-101 | PT-2385
相关库: Anti-Neurodegenerative Disease Compound Library | Drug Repurposing Compound Library | Anti-Cancer Drug Library | Anti-Metabolism Disease Compound Library | Human Metabolite Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Active Compound Library | Metabolism Compound Library | Anti-Viral Compound Library | Anti-Infection Compound Library
Bioactivity
英文名: Oltipraz
描述: Oltipraz (RP 35972) 是一种 Nrf2的强效激活剂。它时间依赖性地抑制 HIF-1α激活，IC50为 10 μM，浓度 ≥ 10 μM 时完全消除 HIF-1α诱导。
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
溶解度: DMSO : 15 mg/mL (66.27 mM)
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: PHD2-IN-1 | SYP-5 | AKBA | Oroxylin A | M1001 | Panaxadiol | HIF-2α-IN-9 | PHD-1-IN-1 | EHP-101 | PT-2385
相关库: Anti-Neurodegenerative Disease Compound Library | Drug Repurposing Compound Library | Anti-Cancer Drug Library | Anti-Metabolism Disease Compound Library | Human Metabolite Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Active Compound Library | Metabolism Compound Library | Anti-Viral Compound Library | Anti-Infection Compound Library
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