Molecular Formula | C19H16N2O3 |
Molar Mass | 320.34 |
Density | 1.17±0.1 g/cm3(Predicted) |
Solubility | DMSO: >10mg/mL |
Appearance | solid |
Color | white to off-white |
pKa | 12.12±0.46(Predicted) |
Storage Condition | 2-8°C |
Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months. |
In vitro study | PNU-74654 binds to β-catenin with a K D of 450 nM. The Tcf3/Tcf4-binding surface on β-catenin contains a well-defined hot spot around residues K435 and R469. The binding mode of PNU-74654 involves the two narrow pockets on either side of this hot spot. In NCI-H295 cells,PNU-74654 significantly decreases cell proliferation 96 h after treatment, increases early and late apoptosis, decreases nuclear beta-catenin accumulation, impairs CTNNB1/beta-catenin expression and increases beta-catenin target genes 48 h after treatment. No effects are observed on HeLa cells. In NCI-H295 cells, PNU-74654 decreases cortisol, testosterone and androstenedione secretion 24 and 48 h after treatment. The SF1 and CYP21A2 mRNA expression as well as the protein levels of STAR and aldosterone synthase are decreased in NCI-H295 cells after 48 h PNU-74654 treatment. In Y1 cells, PNU-74654 impairs corticosterone secretion 24 h after treatment but does not decrease cell viability. |
Hazard Symbols | Xn - Harmful |
Risk Codes | 22 - Harmful if swallowed |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.122 ml | 15.608 ml | 31.217 ml |
5 mM | 0.624 ml | 3.122 ml | 6.243 ml |
10 mM | 0.312 ml | 1.561 ml | 3.122 ml |
5 mM | 0.062 ml | 0.312 ml | 0.624 ml |
biological activity | PNU-74654 is an inhibitor of the Wnt/β-catenin pathway with an IC50 value of 129.8 μm in NCI-H295 cells. |
Target | 129.8 μm (Wnt/β-catenin, NCI-H295 cell) |
in vitro study | PNU-74654 bindings to β-catenin with a K D of 450 nM. The Tcf3/Tcf4-binding surface on β-catenin contains a well-defined hot spot around residues K435 and R469. The binding mode of PNU-74654. In NCI-H295 cells,PNU-74654 significant degradation cell propagation 96 h after treatment, increases early and late apoptosis, decreases nuclear beta-catenin accumulation, impairs CTNNB1/beta-catenin expression and increases beta-catenin target genes 48 h after treatment. No effects are observed on HeLa cells. In NCI-H295 cells, PNU-74654 decreases cortisol testosterone and androstenedione secretion 24 and 48 h after treatment. The SF1 and CYP21A2 mRNA expression as well as the protein levels of STAR and aldosterone synthase are decreased in NCI-H295 cells after 48 h PNU-74654 treatment. In Y1 cells, PNU-74654 impairs corticosterone secretion 24 h after treatment but does not decrease cell viability. |