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Wortmannin (SL-2052) 是一种有效的,不可逆的,选择性PI3K 抑制剂,IC50 值为 3 nM。Wortmannin (SL-2052) 阻断自噬 (autophagy) 形成,并有效抑制 Polo-like kinase 1 (PlK1) 和 Plk3,IC50 值分别为 5.8 和 48 nM。
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更新时间:2026/10/7 8:42:42关注度:2470
关键词标签:SL-2052
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CAS No. : 19545-26⁻⁷
MCE 国际站:Wortmannin
产品活性:Wortmannin (SL-2052) 是一种有效的,不可逆的,选择性PI3K 抑制剂,IC50 值为 3 nM。Wortmannin (SL-2052) 阻断自噬 (autophagy) 形成,并有效抑制 Polo-like kinase 1 (PlK1) 和 Plk3,IC50 值分别为 5.8 和 48 nM。
研究领域:PI3K/Akt/mTOR | Cell Cycle/DNA Damage | Autophagy | Anti-infection
作用靶点:PI3K | Polo-like Kinase (PLK) | Autophagy | Antibiotic
In Vitro: Wortmannin (0-100 nM; 24⁻⁷2 hours) inhibits the proliferation of K562 cells in a time- and dose-dependent manner. The IC50 values at 24 hour, 48 hour, and 72 hour are 25±0.10 nM, 12.5±0.08 nM, and 6.25±0.11 nM, respectively. Wortmannin prevents nuclear entry of YAP.
In Vivo: Wortmannin (oral gavage; daily; in Scid mice; one group of eight mice is dosed with Wortmannin 1 mg/kg for all 14 days. The second group of eight mice is dosed with Wortmannin 1.5 mg/kg for the first 5 days and the dose is decreased to 1 mg/kg for the remaining treatment period) treatment significantly slower the growth rate of murine C3H mammary tumor and human MCF⁻⁷ breast cancer xenograft. A dose of 1 mg/kg Wortmannin for 7 days decrease the tumor burdens in mice with established murine C3H mammary tumors by 54% relative to controls. Human MCF⁻⁷ breast cancer xenograft burdens are decreased by 97% relative to controls after 14 days of 1 mg/kg Wortmannin beginning 1 day after tumor implantation.
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