PRI-724

SKU: orb1685665

Description

PRI-724 is a selective small molecule that disrupts the β-catenin/CBP protein-protein interaction. It is used in cancer research, particularly for studying Wnt/β-catenin signaling pathways, and has been investigated in both in vitro assays and in vivo preclinical models.

Research Area

Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 1422253-38-0
• MW: 658.64
• Purity: 99.11% (May vary between batches)
• Formula: C₃₃H₃₅N₆O₇P
• SMILES: C([C@@H]1N2[C@@](N(C(NCC3=CC=CC=C3)=O)N(C)CC2=O)([C@H](C)N(CC=4C5=C(C=CC4)C=CC=N5)C1=O)[H])C6=CC=C(OP(=O)(O)O)C=C6
• Target: Wnt/beta-catenin
• Solubility: DMSO:55 mg/mL (83.51 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.04 mM);Ethanol:1.8 mg/mL (2.73 mM)

Bioactivity

• 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. 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.
• 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

beta-catenin, betacatenin, bcatenin, C-82 prodrug, Foscenvivint, ICG-001 analog, Wnt/betacatenin, Wnt/b-catenin, Wnt, PRI 724, PRI724, PRI-724, Wnt/β-catenin, βcatenin

Compound Identifiers

PubChem CID

71509318