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经验配方 C₁₇H₁₆N₄O₂S₂ 描述 概述 A cell-permeable thienopyrrolopyridazinone that exhibits good aqueous solubility (29.6 µg/mL or 79.5 µM in PBS, pH 7.4) and acts as a potent allosteric PKM2 activator (AC50 = 92 nM; [PKM2] = 0.1 nM) by stabilizing PKM2 tetramer via stoichiometric interaction with FBP-bound PKM2 (2 activator/4 FBP/tetramer) in a similar manner as PKM2 Activator III (Cat. No. 504537). Reprorted to retard human lung carcinoma H1299 proliferation under hypoxia, but not normoxia, condition in cultures (doubling time = 50 and 35 h, respectively, with or without 30 µM TEPP-46; 1% O2) in vitro and impair H1299 tumorigenesis in mice (50 mg/kg/12 h p.o.) in vivo with no apparent toxicity. 产品目录编号 505487 品牌系列 Calbiochem®
同义词 6-((3-Aminophenyl)methyl)-4-methyl-2-methylsulfinylthieno[3,4]pyrrolo[1,3-d]pyridazin-5-one, Pyruvate Kinase M2 Activator IV, ML265, NCGC00186528, TEPP46 参考 参考 Anastasiou, D., et al. 2012. Nat. Chem. Biol. 8, 839.
Jiang, J.K., et al. 2010. Bioorg. Med. Chem. Lett. 20, 3387.产品信息 形式 White solid Hill配方 C₁₇H₁₆N₄O₂S₂ 化学配方 C₁₇H₁₆N₄O₂S₂ 可逆 Y 结构配方图像 生物信息 主靶 PKM2 纯度 ≥98% by HPLC 理化信息 细胞可渗透 Y 溶解度 DMSO 储存和货运信息 货运代码 Ambient Temperature Only
毒性 Standard Handling
储存 +2°C to +8°C
避光 Protect from light
无需冷冻 No
特殊指南 Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C. 包装信息 惰性气体下包装 Packaged under inert gas
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