产品
编 号：F754537
分子式：C42H41N9O6
分子量：767.83
分子式：C42H41N9O6
分子量：767.83
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CAS No: 2673364-10-6
产品详情
生物活性：
DDO3711, a PP5-recruiting phosphatase recruitment chimeras (PHORCs), is formed by connecting a small molecular apoptosis signal-regulated kinase 1 (ASK1) inhibitor to a PP5 activator through a chemical linker. DDO3711 specifically inhibits ASK1 (IC50 =164.1 nM) not ASK2 (IC50>20 μM). DDO3711 significantly dephosphorylates p-ASK1T838 by recruiting PP5 and shows the ASK1-dependent antiproliferative activity. DDO3711 has anti-cancer activity and has the potential for abnormally phosphorylated oncoproteins research.
体内研究：
DDO3711 (20, 40 mg/kg; 腹腔给药; 每天; 持续 21 天)以剂量依赖性方式显着抑制肿瘤生长。 Animal Model:Four-week-old BALB/c nude mice with MKN45 cells
Dosage:20, 40 mg/kg
Administration:IP; daily; for 21 days
Result:Caused significant inhibition of tumor growth in a dose-dependent manner. Significantly decreased the level of p-ASK1T838.
体外研究：
DDO3711 (15 μM; 24小时) 通过以 PP5 依赖性方式减少 p-ASK1T838，从而对胃癌细胞显示出抗增殖作用。DDO3711 不抑制 GES-1 细胞和 HGC-27 细胞的增殖。 DDO3711 (5 μM; 1-24小时) 以浓度依赖性方式抑制 CDK4/6 和细胞周期蛋白 D1 的表达。 DDO3711 (5-50 μM; 0.5-2 小时) 在体外和细胞中有效地使 p-ASK1T838 去磷酸化。DDO3711 浓度依赖性降低 p-JNK 和 p-p38 的水平。
DDO3711, a PP5-recruiting phosphatase recruitment chimeras (PHORCs), is formed by connecting a small molecular apoptosis signal-regulated kinase 1 (ASK1) inhibitor to a PP5 activator through a chemical linker. DDO3711 specifically inhibits ASK1 (IC50 =164.1 nM) not ASK2 (IC50>20 μM). DDO3711 significantly dephosphorylates p-ASK1T838 by recruiting PP5 and shows the ASK1-dependent antiproliferative activity. DDO3711 has anti-cancer activity and has the potential for abnormally phosphorylated oncoproteins research.
体内研究：
DDO3711 (20, 40 mg/kg; 腹腔给药; 每天; 持续 21 天)以剂量依赖性方式显着抑制肿瘤生长。 Animal Model:Four-week-old BALB/c nude mice with MKN45 cells
Dosage:20, 40 mg/kg
Administration:IP; daily; for 21 days
Result:Caused significant inhibition of tumor growth in a dose-dependent manner. Significantly decreased the level of p-ASK1T838.
体外研究：
DDO3711 (15 μM; 24小时) 通过以 PP5 依赖性方式减少 p-ASK1T838，从而对胃癌细胞显示出抗增殖作用。DDO3711 不抑制 GES-1 细胞和 HGC-27 细胞的增殖。 DDO3711 (5 μM; 1-24小时) 以浓度依赖性方式抑制 CDK4/6 和细胞周期蛋白 D1 的表达。 DDO3711 (5-50 μM; 0.5-2 小时) 在体外和细胞中有效地使 p-ASK1T838 去磷酸化。DDO3711 浓度依赖性降低 p-JNK 和 p-p38 的水平。
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