PRI-724

Catalog No.S8968 Batch:S896801

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Technical Data

Formula
C33H35N6O7P
Molecular Weight 658.64 CAS No. 1422253-38-0
Solubility (25°C)* In vitro DMSO 100 mg/mL (151.82 mM)
Ethanol 2 mg/mL (3.03 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description PRI-724 (C-82 prodrug, ICG-001 analog) is a potent and specific inhibitor that disrupts the interaction of β-catenin and CBP.
Targets
β-catenin [1] CBP [1]
In vivo

PRI-724 reduces liver fibrosis,and hepatic hydroxyproline levels, in HCV mice while attenuating αSMA induction. PRI-724 leads to increased levels of matrix metalloproteinase (MMP)-8 mRNA in the liver, along with elevated levels of intrahepatic neutrophils and macrophages/monocytes. In conclusion, PRI-724 ameliorates HCV-induced liver fibrosis in mice. PRI-724 is a drug candidate which possesses antifibrotic effect.[1]

Protocol (from reference)

Cell Assay:

[2]
  • Cell lines

    SCC-25 cells

  • Concentrations

    0.85 µM

  • Incubation Time

    48 h

  • Method

    Cells were treated with various concentrations of PRI-724.
Animal Study:

[1]
  • Animal Models

    HCV GT1b transgenic mice (MxCre+/−/CN2-29+/−)

  • Dosages

    5 mg/kg, 15 mg/kg, 20 mg/kg; 1 mg/kg

  • Administration

    IP/SC

Selleck's PRI-724 has been cited by 29 publications

MEN1 Deficiency-Driven Activation of the β-Catenin-MGMT Axis Promotes Pancreatic Neuroendocrine Tumor Growth and Confers Temozolomide Resistance [ Adv Sci (Weinh), 2024, 11(35):e2308417] PubMed: 39041891
Retinoic acid enhances HIV-1 reverse transcription and transcription in macrophages via mTOR-modulated mechanisms [ Cell Rep, 2024, 43(7):114414] PubMed: 38943643
Gain-of-function mutant p53 together with ERG proto-oncogene drive prostate cancer by beta-catenin activation and pyrimidine synthesis [ Nat Commun, 2023, 14(1):4671] PubMed: 37537199
Stromal-induced epithelial-mesenchymal transition induces targetable drug resistance in acute lymphoblastic leukemia [ Cell Rep, 2023, 42(7):112804] PubMed: 37453060
β-catenin-IRP2-primed iron availability to mitochondrial metabolism is druggable for active β-catenin-mediated cancer [ J Transl Med, 2023, 21(1):50] PubMed: 36703130
Combinations of PRI-724 Wnt/β-Catenin Pathway Inhibitor with Vismodegib, Erlotinib, or HS-173 Synergistically Inhibit Head and Neck Squamous Cancer Cells [ Int J Mol Sci, 2023, 24(13)10448] PubMed: 37445628
Critical role for ribonucleoside-diphosphate reductase subunit M2 in ALV-J-induced activation of Wnt/β-catenin signaling via interaction with P27 [ J Virol, 2023, 97(8):e0026723] PubMed: 37582207
Machine learning on large scale perturbation screens for SARS-CoV-2 host factors identifies β-catenin/CBP inhibitor PRI-724 as a potent antiviral [ Front Microbiol, 2023, 14:1193320] PubMed: 37342561
PRI-724 and IWP-O1 Wnt Signaling Pathway Inhibitors Modulate the Expression of Glycolytic Enzymes in Tongue Cancer Cell Lines [ Curr Issues Mol Biol, 2023, 45(12):9579-9592] PubMed: 38132445
CDK7/12/13 inhibition targets an oscillating leukemia stem cell network and synergizes with venetoclax in acute myeloid leukemia [ EMBO Mol Med, 2022, e14990] PubMed: 35253392

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.