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PNU-74654 (PNU74654) is a novel inhibitor of Wnt/β-catenin pathway (IC50 = 129.8 μM), acting by inhibiting the interaction between ß-catenin and T cell factor 4 (Tcf4), and disrupting the Wnt signaling pathway.
| ln Vitro |
PNU-74654 has a 450 nM KD for binding β-catenin. A distinct hotspot is present on the Tcf3/Tcf4 binding surface of β-catenin, specifically at residues K435 and R469. Two little pockets on either side of this hotspot are part of the binding design of PNU-74654 [2]. PNU-74654 dramatically inhibited cell proliferation, enhanced early and late cell counts, decreased nuclear β-catenin accumulation, hampered CTNNB1/β-catenin expression 96 hours post-treatment, and enhanced early and late cell counts 48 hours post-treatment in NCI-H295 cells. Hours rise in target genes of β-catenin. On HeLa cells, no impacts were seen. PNU-74654 lowers amygdalone and soy alcohol in NCI-H295 cells 24 and 48 hours after treatment. STAR, aldosterone synthase protein, and SF1 and CYP21A2 mRNA expression in NCI-H295 cells following a 48-hour treatment period. level falls. PNU-74654 decreases corticosterone in Y1 cells 24 hours post-treatment, but does not lower cell survival [1].
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| References |
[1]. Leal LF, et al. Inhibition of the Tcf/beta-catenin complex increases apoptosis and impairs adrenocortical tumor cell proliferation and adrenal steroidogenesis. Oncotarget. 2015 Dec 15;6(40):43016-32.
[2]. Trosset JY, et al. Inhibition of protein-protein interactions: the discovery of druglike beta-catenin inhibitors by combining virtual and biophysical screening. Proteins. 2006 Jul 1;64(1):60-7 |
| Molecular Formula |
C19H16N2O3
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|---|---|
| Molecular Weight |
320.348
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| CAS # |
113906-27-7
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| Related CAS # |
113906-27-7;
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| SMILES |
O=C(N/N=C/C1=CC=C(C)O1)C2=CC=CC=C2OC3=CC=CC=C3
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 30 mg/mL (~93.65 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.80 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.80 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1216 mL | 15.6079 mL | 31.2159 mL | |
| 5 mM | 0.6243 mL | 3.1216 mL | 6.2432 mL | |
| 10 mM | 0.3122 mL | 1.5608 mL | 3.1216 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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