Molecular Weight(MW): 548.63
PRI-724 is a potent, specific inhibitor of the canonical Wnt signaling pathway in cancer stem cells with potential antineoplastic activity. PRI-724 specifically inhibits the recruiting of beta-catenin with its coactivator CBP.
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Lpcat3KD 3T3L1 pre-adipocytes were treated with different concentration of Wnt/-catenin pathway inhibitors and then underwent differentiation. The fully differentiated cells were collected. Triglyceride, free cholesterol, and total cholesterol were measured. IWR-1-endo (IC50=180nM) inhibits Wnt-induced stabilization of β-catenin by acting on the target of β-catenin destruction complex in cytosol; PRI-724 (IC50=150 nM) and ICG-001 (IC50=3 μM) inhibit the recruiting of β-catenin with its coactivator element-binding protein(CBP) in nucleus. Values are mean ± SD, n = 3. Bars labeled with different uppercase letters are statistically different (p < 0.05).
Biochim Biophys Acta Mol Cell Biol Lipids, 2018, 1863(8):834-843. PRI-724 purchased from Selleck.
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Choose Selective Wnt/beta-catenin Inhibitors
|Description||PRI-724 is a potent, specific inhibitor of the canonical Wnt signaling pathway in cancer stem cells with potential antineoplastic activity. PRI-724 specifically inhibits the recruiting of beta-catenin with its coactivator CBP.|
PRI-724 binds specifically to CBP but not the related transcriptional coactivator p300, thereby disrupting the interaction of CBP with β-catenin. Treatment with PRI-724 selectively induces apoptosis in colon carcinoma cells but not in normal colonic epithelial cells and reduces in vitro growth of colon carcinoma cells.
|In vivo||PRI-724 exhibits antitumor activity in the mouse xenograft models of colon cancer. The initial results of the Phase I clinic trial of PRI-724 has been disclosed publically. The drug exhibits an acceptable toxicity profile with only one dose-limiting toxicity of grade 3 reversible hyperbilirubinaemia. An Open-Label dose-escalation phase I/II study of PRI-724 for patients with advanced myeloid malignancies is still ongoing.|
|In vitro||DMSO||100 mg/mL (182.27 mM)|
|Ethanol||100 mg/mL (182.27 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.
* 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.
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This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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Frequently Asked Questions
How to reconstitute the compound (S8262) for in vivo studies?
S8262 can be dissolved in 2% DMSO+30% PEG 300+5% Tween 80+ddH2O as clear solution up tp 5mg/ml.