b-Catenin/Tcf Inhibitor II, PKF118-310 (1,6-Dimethylpyrimido[5,6-e][1,2,4]triazine-5,7-dione, Wnt Pathway Inhibitor IV)

Size

£372.00

SKU:: 217207
Molecular Weight:: 193.2
Purity:: ~95% (HPLC)
Storage Conditions:: -20°C
Supplier:: United States Biological
Format:: Supplied as a dark yellow solid.
Extra Details:: A synthetic cell-permeable actinobacteria pyrimidotriazine-dione that selectively disrupts b-catenin-Tcf4 interaction (IC50=0.8uM in cell-free binding assays) and inhibits b-catenin-regulated cellular transcription activity (IC50=0.3uM in HCT116-based reporter assays). PKF118-310 is demonstrated to reverse b-catenin, but not siamois, mRNA-induced ventral body axis formation in Xenopus embryos, while direct tumor site injection (1mg/kg/0.5 wk) in HepG2 xenograph mice is shown to increase the number of apoptotic cells and decrease the expression of b-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. Formula: C7H7N5O2 Molecular Weight: 193.2 Solubility: DMSO (100mg/ml) Storage and Stability: Lyophilized powder may be stored at -20°C. Stable for 12 months at -20°C. Reconstitute with sterile buffer or dH2O. Aliquot to avoid repeated freezing and thawing. Store at -20°C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.