PRI-724, also known as C-82 prodrug/ICG-001 analog, is a potent, specific inhibitor of the canonical Wnt signaling pathway in cancer stem cells with potential antineoplastic activity. Wnt signaling pathway inhibitor PRI-724 specifically inhibits the recruiting of beta-catenin with its coactivator CBP (the binding protein of the cAMP response element-binding protein CREB); together with other transcription factors beta-catenin/CBP binds to WRE (Wnt-responsive element) and activates transcription of a wide range of target genes of Wnt/beta-catenin signaling. Note: Chemical structures of ICG-001 and PRR-724 look very close, but they are not the same molecule. Many vendors confused them.
CAS Number: 1422253-38-0
Molecular Weight: 658.64
Related CAS Number:
Chemical Name: (6S,9S,9aS)-Hexahydro-2,9-dimethyl-4,7-dioxo-N-(phenylmethyl)-6-[[4-(phosphonooxy)phenyl]methyl]-8-(8-quinolinylmethyl)-2H-pyrazino[2,1-c][1,2,4]triazine-1(6H)-carboxamide
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Soluble in DMSO, not in water
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥360 days if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
PRI-724 is phosphorylated-C-82 and is rapidly hydrolyzed to its active form C-82 in vivo. PRI-724 treatment reduces the fibrosis induced by CCl4 or BDL. C-82, an active form of PRI-724, inhibits the activation of isolated primary mouse quiescent hepatic stellate cells (HSCs) and promotes cell death in culture-activated HSCs.
- Okazaki H, Sato S, Koyama K, Morizumi S, Abe S, Azuma M, Chen Y, Goto H, Aono Y, Ogawa H, Kagawa K, Nishimura H, Kawano H, Toyoda Y, Uehara H, Kouji H, Nishioka Y. The novel inhibitor PRI-724 for Wnt/β-catenin/CBP signaling ameliorates bleomycin-induced pulmonary fibrosis in mice. Exp Lung Res. 2019 Jul 12:1-12. doi: 10.1080/01902148.2019.1638466. [Epub ahead of print] PubMed PMID: 31298961.
- Rao P, Pang M, Qiao X, Yu H, Wang H, Yang Y, Ren X, Hu M, Chen T, Cao Q, Wang Y, Khushi M, Zhang G, Wang YM, Heok P'ng C, Nankivell B, Lee VW, Alexander SI, Zheng G, Harris DC. Promotion of β-catenin/Foxo1 signaling ameliorates renal interstitial fibrosis. Lab Invest. 2019 Jun 26. doi: 10.1038/s41374-019-0276-z. [Epub ahead of print] PubMed PMID: 31243340.
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- Kleszcz R, Szymańska A, Krajka-Kuźniak V, Baer-Dubowska W, Paluszczak J. Inhibition of CBP/β-catenin and porcupine attenuates Wnt signaling and induces apoptosis in head and neck carcinoma cells. Cell Oncol (Dordr). 2019 Aug;42(4):505-520. doi: 10.1007/s13402-019-00440-4. Epub 2019 May 14. PubMed PMID: 31089983.
- Bocchicchio S, Tesone M, Irusta G. Convergence of Wnt and Notch signaling controls ovarian cancer cell survival. J Cell Physiol. 2019 May 13. doi: 10.1002/jcp.28775. [Epub ahead of print] PubMed PMID: 31087357.
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