Quality Segment
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
-10 to -25°C
SMILES string
O=C(NCC1=CC=CC=C1)N(N(CC2=O)C)[C@]([C@@H](N(C3=O)CC4=CC=CC5=C4N=CC=C5)C)([H])N2[C@H]3CC6=CC=C(C=C6)OP(O)(O)=O
General description
PRI-724 (Foscenvivint; OP-724) is a phosphorylated predrug that is hydrolyzed to the ICG-001 analog C-82, a selective inhibitor against β-catenin interaction with CREB-binding protein (CBP; CREBBP), but not p300, resulting in upregulated p300/β-catenin complex. PRI-724 treatment reduces the fibrosis induced by CCl4 (1:4 v/v in mineral oil, 1mL/kg 2x per wk) or bile duct ligation (BDL) in mice in vivo (0.4 mg in PBS/kg i.p. 4x per wk). PRI-724 active metabolite C-829 (10 µM) inhibits β-catenin signaling in isolated primary hepatic stellate cells (HSCs) from mice in cultures. PRI-724 inhibits the transcriptional activity of β-catenin by preventing its interaction with CBP. This inhibition leads to a decrease in the transcription of target genes that are normally activated by the β-catenin/CBP interaction. Studies have demonstrated that PRI-724 not only inhibits cell proliferation in models of hepatocellular carcinoma (HCC) but also induces apoptosis and alters cell cycle dynamics.
Application
PRI-724 has been used:
- to inhibit Wnt signaling pathways and study its anti-tumor activity in hepatocellular carcinoma
- to study its effects in non alcoholic steatohepatitis (NASH)-related liver fibrosis
- to study its role ininhibiting viral replication in the context of SARS-CoV-2
Biochem/physiol Actions
Precursor form of the ICG-001 analog C-82, a selective inhibitor against β-catenin interaction with CREB-binding protein (CBP; CREBBP), but not p300.
hcodes
signalword
Warning
Hazard Classifications
Acute Tox. 4 Oral
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable