DASA-58
货号:
13941-1mg 基本售价:
490.0 元 规格:
1 mg
产品信息
概述货号 | 13941-1mg |
描述 | DASA-58 is a selective activator of pyruvate kinase M2 (PKM2; AC50 = 38 nM in vitro, EC50 = 19.6 µM in cells).1 DASA-58 converts PKM2 to a constitutively active enzyme state that is resistant to inhibition by tyrosine-phosphorylated proteins.1 Through its effects on PKM2, DASA-58 blocks the induction of HIF-1α by lipopolysaccharide in bone marrow-derived macrophages, suppressing the expression of several HIF-1α-dependent targets, including IL-1β.2 It also impairs metastatic dissemination of prostate cancer PCa cells in SCID mice.3 |
别名 | ML-203;NCGC00185916; |
性能供应商 | Cayman |
应用文献 |
1.Anastasiou, D.,Yu, Y.,Israelsen, W.J., et al. Pyruvate kinase M2 activators promote tetramer formation and suppress tumorigenesis. Nature Chemical Biology 8, 839-847 (2012). 2.Palsson-McDermott, E.M.,Curtis, A.M.,Goel, G., et al. Pyruvate kinase M2 regulates Hif-1α activity and IL-1β induction and is a critical determinant of the warburg effect in LPS-activated macrophages. Cell.Metab. 21(1), 65-80 (2015). 3.Giannoni, E.,Taddei, M.L.,Morandi, A., et al. Targeting stromal-induced pyruvate kinase M2 nuclear translocation impairs oxphos and prostate cancer metastatic spread. Oncotarget 6(27), 24061-24074 (2015).
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运输条件 | Wet ice in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥98% |
计算分子量 | 453.5 |
分子式 | C19H23N3O6S2 |
CAS号 | 1203494-49-8 |
稳定性 | ≥ 2 years |
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