219331

β-Catenin/Tcf Inhibitor II, PKF118-310

The β-Catenin/Tcf Inhibitor II, PKF118-310 controls the biological activity of β-Catenin/Tcf. This small molecule/inhibitor is primarily used for Cancer applications.

• Synonym(s): β-Catenin/Tcf Inhibitor II, PKF118-310, 1,6-Dimethylpyrimido[5,6-e][1,2,4]triazine-5,7-dione, Wnt Pathway Inhibitor X
• Empirical Formula (Hill Notation): C₇H₇N₅O₂
• Molecular Weight: 193.16
• UNSPSC Code: 12352200
• NACRES: NA.77
• MDL number: MFCD00459812
• Assay: ≥95% (HPLC)
• Form: solid
• Storage condition: OK to freeze, protect from light

Properties

• Quality Segment: 100
• assay: ≥95% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze, protect from light
• color: dark yellow
• solubility: DMSO: 100 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C
• SMILES string: N1(N=CN=C2C1=NC(=O)N(C2=O)C)C
• InChI: 1S/C7H7N5O2/c1-11-6(13)4-5(10-7(11)14)12(2)9-3-8-4/h3H,1-2H3
• InChI key: SLGRAIAQIAUZAQ-UHFFFAOYSA-N

Description

General description

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.

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Wei, W., et al. 2010. Int. J. Cancer126, 2426.
Lepourcelet, M., et al. 2004. Cancer Cell5, 91.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

Safety Information

• pictograms: GHS06
• signalword: Danger
• hcodes: H300
• pcodes: P264 - P270 - P301 + P310 - P405 - P501
• Hazard Classifications: Acute Tox. 2 Oral
• Storage Class: 6.1A - Combustible acute toxic Cat. 1 and 2 / very toxic hazardous materials
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable