PRI-724

製品コードS8968 バッチS896801

化学情報

	Synonyms	C-82 prodrug, ICG-001 analog	Storage (From the date of receipt)	3 years -20°C powder
	化学式	C₃₃H₃₅N₆O₇P
	分子量	658.64	CAS No.	1422253-38-0
Solubility (25°C)*	体外	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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	PRI-724 (C-82 prodrug, ICG-001 analog) is a potent and specific inhibitor that disrupts the interaction of β-catenin and CBP.
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]

製品説明

PRI-724 (C-82 prodrug, ICG-001 analog) is a potent and specific inhibitor that disrupts the interaction of β-catenin and CBP.

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]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	SCC-25 cells
	濃度	0.85 µM
	反応時間	48 h
	実験の流れ	Cells were treated with various concentrations of PRI-724.
動物実験	動物モデル	HCV GT1b transgenic mice (MxCre^+/−/CN2-29^+/−)
	投薬量	5 mg/kg, 15 mg/kg, 20 mg/kg; 1 mg/kg
	投与方法	IP/SC

参考

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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
The Wnt Signaling Pathway Inhibitors Improve the Therapeutic Activity of Glycolysis Modulators against Tongue Cancer Cells [ Int J Mol Sci, 2022, 23-31248]	PubMed: 35163171
Periostin Augments Vascular Smooth Muscle Cell Calcification via β-Catenin Signaling [ Biomolecules, 2022, 12(8)1157]	PubMed: 36009051

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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