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β-Catenin/Tcf Inhibitor II, PKF118-310
1,6-Dimethylpyrimido[5,6-e][1,2,4]triazine-5,7-dione, Wnt Pathway Inhibitor X
A synthetic cell-permeable actinobacteria pyrimidotriazine-dione that selectively disrupts β-catenin-Tcf4 interaction (IC50 = 0.8 µM in cell-free binding assays) and inhibits β-catenin-regulated cellular transcription activity (IC50 = 0.3 µM in HCT116-based reporter assays). PKF118-310 is demonstrated to reverse β-catenin, but not siamois, mRNA-induced ventral body axis formation in Xenopus embryos, while direct tumor site injection (1 mg/kg/0.5 wk) in HepG2 xenograph mice is shown to increase the number of apoptotic cells and decrease the expression of β-catenin target genes (cyclin D1, c-Myc, survivin) in the tumor mass, resulting in an effective tumor growth retardation (by ~60% after a 4-wk treatment period) in vivo.
产品信息
Form Dark yellow solid
Molar mass 193.2
Protect from Light 是的
Packaged under inert gas 是的
Purity ≥95% by HPLC
Solubility DMSO
Chemical formula C7H7N5O2
商店和运输信息
Storage +2°C to +8°C
Ship Ambient Temperature Only
Standard Handling |