| Name | PRI-724 |
| Description | PRI-724 is a second-generation, selective small molecule inhibitor of the β-catenin/CBP interaction. |
| In vitro | METHODS: CAL27 and FaDu cells were treated with HS-173, erlotinib, and PRI-724 (0-100 μM, 48 hours), and cell viability was analyzed by resazurin assay.
RESULTS The combination of PRI-724 and HS-173 synergistically reduced the viability of FaDu cells; in CAL27 cells, the best inhibitory results were observed with the mixture of PRI-724 and erlotinib. [2] |
| In vivo | METHODS: HCV transgenic mice were treated with PRI-724 (5, 20 mg/kg, intraperitoneally, once a day, for 6 weeks) intraperitoneally, and the antifibrotic activity of PRI-724 against HCV-induced liver fibrosis was evaluated.
RESULTS In HCV transgenic mice, the expression of S100A4, which is controlled by CBP/β-catenin, was increased; this induction was attenuated by the administration of PRI-724, and the HCV-induced increase in hepatic hydroxyproline was also attenuated. Inhibition of CBP/β-catenin by PRI-724 is effective against HCV-induced liver fibrosis. [1]
METHODS: HCV transgenic mice were treated with PRI-724 (0.1, 0.3, 1 mg/kg, subcutaneous injection, 6 weeks) to evaluate the anti-fibrotic activity of PRI-724.
RESULTS PRI-724 can effectively reduce the area of collagen fibers in the liver in a dose-dependent manner and increase the expression level of Mmp8 mRNA and the number of F4/80, Ly-6C and Gr-1 positive cells. [1] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 150 mg/mL (227.74 mM), Sonication is recommended. Ethanol : 1.8 mg/mL (2.73 mM), Sonication is recommended. 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (3.04 mM), Sonication is recommended.
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| Keywords | βcatenin | Wnt/β-catenin | Wnt/betacatenin | Wnt/b-catenin | Wnt | PRI-724 | PRI724 | PRI 724 | beta-catenin | betacatenin | bcatenin |
| Inhibitors Related | Chlorquinaldol | Urea | Wnt pathway activator 1 | Neohesperidin | XAV-939 | Ethyl linoleate | Monensin sodium salt | Nimbolide | Isoquercetin | (±)-Nornicotine | Methyl Vanillate | Bisdemethoxycurcumin |
| Related Compound Libraries | Failed Clinical Trials Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Hematonosis Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Neuroprotective Compound Library | Inhibitor Library | Bioactive Compounds Library Max | Wnt/Hedgehog/Notch Compound Library | Anti-Cancer Active Compound Library | Anti-Cancer Drug Library |