PNU-74654
Based on 12 publication(s) in Google Scholar
PNU-74654 is an inhibitor of Wnt/β-catenin pathway with an IC50 of 129.8 μM in NCI-H295 cell.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 99.86%
- CAS No.: 113906-27-7
- 화학식: C19H16N2O3
- 분자량:320.34
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) PNU-74654
More- J Cell Physiol. 2019 Sep;234(9):15472-15486. [Abstract]
- Heliyon. 2024 Feb 5;10(4):e24644. [Abstract]
- Environ Toxicol. 2020 Jun;35(6):697-706. [Abstract]
- Curr Issues Mol Biol. 2022 Jan 4;44(1):222-232. [Abstract]
- PeerJ. 2023 Aug 18:11:e15841. [Abstract]
- Medicina (Kaunas). 2023 Aug 24;59(9):1531. [Abstract]
- Medicina (Kaunas). 2022 Jun 14;58(6):798. [Abstract]
- Exp Ther Med. 2022 Apr;23(4):302. [Abstract]
- J Mol Histol. 2025 Apr 26;56(3):144. [Abstract]
- Stem Cells Dev. 2021 Aug 15;30(16):806-815. [Abstract]
- bioRxiv. 2026 Jun 9.
- Res Sq. 2024 Sep 02.
Customer Validation & Images
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WB
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WB
Biological Activity
129.8 μM (Wnt/β-catenin, NCI-H295 cell)[1]
PNU-74654 binds to β-catenin with a KD of 450 nM. The Tcf3/Tcf4-binding surface on β-catenin contains a well-defined hot spot around residues K435 and R469. The binding mode of PNU-74654 involves the two narrow pockets on either side of this hot spot[2]. In NCI-H295 cells,PNU-74654 significantly decreases cell proliferation 96 h after treatment, increases early and late apoptosis, decreases nuclear beta-catenin accumulation, impairs CTNNB1/beta-catenin expression and increases beta-catenin target genes 48 h after treatment. No effects are observed on HeLa cells. In NCI-H295 cells, PNU-74654 decreases cortisol, testosterone and androstenedione secretion 24 and 48 h after treatment. The SF1 and CYP21A2 mRNA expression as well as the protein levels of STAR and aldosterone synthase are decreased in NCI-H295 cells after 48 h PNU-74654 treatment. In Y1 cells, PNU-74654 impairs corticosterone secretion 24 h after treatment but does not decrease cell viability[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 113906-27-7
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Appearance Solid
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분자량 320.34
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화학식 C19H16N2O3
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Color White to off-white
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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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (12)
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Journal Impact Factor
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Most Recent
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J Cell Physiol
PLCε knockdown overcomes drug resistance to androgen receptor antagonist in castration-resistant prostate cancer by suppressing the wnt3a/β-catenin pathway. [Abstract]2019 Sep;234(9):15472-15486. PMID: 30684266
PNU-74654 purchased from MedChemExpress. Usage Cited in: J Cell Physiol. 2019 Sep;234(9):15472-15486. [Abstract]
Western blot analysis was used to confirm the total protein expression of β-catenin and AR in the LNCaP, DRCaP, BRCaP, and ERCaP cells treated with the wnt/β-catenin activator (AZD2858, 5 nM, 48 hr) or the wnt/β-catenin inhibitor (PNU74654, 129.8 μM, 48 hr).
PNU-74654 purchased from MedChemExpress. Usage Cited in: J Cell Physiol. 2019 Sep;234(9):15472-15486. [Abstract]
Western blot analysis was used to confirm the cytoplasmic and nuclear protein expression of β-catenin and AR in the LNCaP, DRCaP, BRCaP, and ERCaP cells treated with the wnt/β-catenin activator (AZD2858, 5 nM, 48 hr) or the wnt/β-catenin inhibitor (PNU74654, 129.8 μM, 48 hr).
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Heliyon
Astragalus polysaccharide improves diabetic ulcers by promoting M2-polarization of macrophages to reduce excessive inflammation via the β-catenin/ NF-κB axis at the late phase of wound-healing. [Abstract]2024 Feb 5;10(4):e24644. PMID: 38390059 -
Environ Toxicol
2020 Jun;35(6):697-706. PMID: 31995275 -
Curr Issues Mol Biol
PNU-74654 Suppresses TNFR1/IKB Alpha/p65 Signaling and Induces Cell Death in Testicular Cancer. [Abstract]2022 Jan 4;44(1):222-232. PMID: 35723395 -
PeerJ
Transcription factor EB (TFEB) improves ventricular remodeling after myocardial infarction by inhibiting Wnt/ β-catenin signaling pathway. [Abstract]2023 Aug 18:11:e15841. PMID: 37609444 -
Medicina (Kaunas)
2023 Aug 24;59(9):1531. PMID: 37763649 -
Medicina (Kaunas)
The Therapeutic Role of PNU-74654 in Hepatocellular Carcinoma May Involve Suppression of NF-κB Signaling. [Abstract]2022 Jun 14;58(6):798. PMID: 35744061 -
Exp Ther Med
Shp2 suppresses fat accumulation in white adipose tissue by activating Wnt/β-catenin signaling following vertical sleeve gastrectomy in obese rats with type-2 diabetes. [Abstract]2022 Apr;23(4):302. PMID: 35340882 -
J Mol Histol
Identification of the oncogenic role of centromere protein M in non-small cell lung cancer via CDC20/MYBL2/Wnt signaling pathways. [Abstract]2025 Apr 26;56(3):144. PMID: 40285932 -
Stem Cells Dev
PDCD4 Negatively Regulated Osteogenic Differentiation and Bone Defect Repair of Mesenchymal Stem Cells Through GSK-3β/β-Catenin Pathway. [Abstract]2021 Aug 15;30(16):806-815. PMID: 34088227 -
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용액&용해도
DMSO : 100 mg/mL (312.17 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.80 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
The PNU-74654 compound is dissolved in DMSO at stock concentrations of 31.2 mM. For working solutions, PNU-74654 is diluted 100X in growth medium with no serum deprivation. NCI-H295 cells are plated at 200,000 cells per well in 24-well plates for gene expression, protein analysis and adrenal steroid measurements. After 48 h, cells are treated with vehicle (0.1%-0.4% DMSO) or 10, 50, 100 and 200 μM PNU-74654. After 24 and 48 h, medium supernatants are collected for adrenal steroid measurements[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
순도&문서
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Data Sheet (274 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.1217 mL | 15.6084 mL | 31.2168 mL | 78.0421 mL |
| 5 mM | 0.6243 mL | 3.1217 mL | 6.2434 mL | 15.6084 mL | |
| 10 mM | 0.3122 mL | 1.5608 mL | 3.1217 mL | 7.8042 mL | |
| 15 mM | 0.2081 mL | 1.0406 mL | 2.0811 mL | 5.2028 mL | |
| 20 mM | 0.1561 mL | 0.7804 mL | 1.5608 mL | 3.9021 mL | |
| 25 mM | 0.1249 mL | 0.6243 mL | 1.2487 mL | 3.1217 mL | |
| 30 mM | 0.1041 mL | 0.5203 mL | 1.0406 mL | 2.6014 mL | |
| 40 mM | 0.0780 mL | 0.3902 mL | 0.7804 mL | 1.9511 mL | |
| 50 mM | 0.0624 mL | 0.3122 mL | 0.6243 mL | 1.5608 mL | |
| 60 mM | 0.0520 mL | 0.2601 mL | 0.5203 mL | 1.3007 mL | |
| 80 mM | 0.0390 mL | 0.1951 mL | 0.3902 mL | 0.9755 mL | |
| 100 mM | 0.0312 mL | 0.1561 mL | 0.3122 mL | 0.7804 mL |
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