SCH529074
Based on 3 publication(s) in Google Scholar
SCH529074 is a potent and orally active p53 activator. SCH529074 binds specifically and conformation-dependently to p53 DBD ( DNA binding domain) with a Ki of 1-2 μM in a saturable manner. SCH529074 restores mutant p53 function and interrupts HDM2-mediated ubiquitination of wild Type p53. SCH529074 can be used for the study of non-small-cell lung carcinoma (NSCLC).
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- Pureté: 99.73%
- CAS No.: 922150-11-6
- Formule: C31H36Cl2N6
- Masse moléculaire:563.56
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) SCH529074
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Customer Validation & Images
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RT-PCR
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WB
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Cell Migration/Invasion Assay
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Flow Cytometry
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Histological Imaging/Staining
Activité biologique
Ki: 1-2 μM (p53 DBD)[2]
SCH529074 (2-4 μM; 24 hours) causes significant reduction in cell viability, it causes a significant decreasing to 20-25% in p53 mutant cells (H157, H1975 and H322) and to 68% in the p53 WT cell line A549 at 4 μM[1].SCH 529074 (2 and 4 μM) induces NSCLC cells (H157, A549, HCT116 and HCT116 p53-/-) arrested at the G0/G1 phase (59%; 72%; 66%; and 57%) compared with the control cells following low concentration (2 μM) of treatment[1].SCH 529074 (2-4 μM; 24 hours) induces the early and late apoptotic rates at 2 μM in H1975 cells. In H157 cells, SCH 529074 treatment induces early and late apoptosis. Similarly, in A549 cells, 2 and 4 μM of SCH 529074 significantly increased early and late apoptosis. In line with that, in colon cancer cells, in HCT116 cells, 4 μM of SCH 529074 causes a significant induction of early and late apoptosis, and 4 μM of SCH 529074 significantly induces early apoptosis in HCT116 p53-/- cells[1].SCH 529074 (2-6 μM; 24 hours) increases?the protein levels of PUMA and p21 revealed to 4 or 6 μM in the cancer cell lines regardless of their p53 status[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:p53 mutant cells (H157, H1975 and H322) and p53 WT cell line A549
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Concentration:2 µM; 4 µM
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Incubation Time:24 hours
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Result:Inhibited cancer WT and mutant cell viability.
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Cell Line:H1975, H157, A549, HCT116, HCT116 p53-/- cells
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Concentration:2 µM, 4 µM, 6 µM
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Incubation Time:24 hours
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Result:Induced apoptosis in all assessed NSCLC cell lines irrespective of their p53 mutational status.
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Cell Line:H1975, H322, H157, A549, HCT116, HCT116 p53-/-
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Concentration:2 µM, 4 µM, 6 µM
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Incubation Time:24 hours
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Result:Increased PUMA and p21 protein expression.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female nude mice, 5–7 weeks of age, received subcutaneous inoculation of DLD-1 human colorectal carcinoma cells[2]
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Dosage:30 or 50 mg/kg
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Administration:Oral administration; twice daily; 4 weeks; started on day 3 until day 31
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Result:Inhibited tumor growth
Chemical Information
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CAS No. 922150-11-6
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Appearance Solid
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Masse moléculaire 563.56
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Formule C31H36Cl2N6
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Color Off-white to light yellow
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SMILES
CN(C)CCCNC1=C2C=CC=CC2=NC(CN3CCN(C(C4=CC=C(Cl)C=C4)C5=CC=C(Cl)C=C5)CC3)=N1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (3)
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Journal Impact Factor
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Most Recent
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Sci Rep
Muscone suppresses inflammation and senescence of nucleus pulposus via p53 signalling during intervertebral disc degeneration. [Abstract]2025 Aug 14;15(1):29794. PMID: 40813817
SCH529074 purchased from MedChemExpress. Usage Cited in: Sci Rep. 2025 Aug 14;15(1):29794. [Abstract]
The mRNA levels of ACAN, CHSY1 and COL2 expression in degenerated NP cell (induced by IL-1β) were measured by qPCR analysis. SCH529074 (2 μM) is the p53 agonist.
SCH529074 purchased from MedChemExpress. Usage Cited in: Sci Rep. 2025 Aug 14;15(1):29794. [Abstract]
Western Blot analysis showing the protein levels of ACAN, COL2, CHSY1 and GAPDH expression treated with SCH529074 (2 μM).
SCH529074 purchased from MedChemExpress. Usage Cited in: Sci Rep. 2025 Aug 14;15(1):29794. [Abstract]
The cell migration in different groups was evaluated by Matrigel coated Transwell invasion assay treated with SCH529074 (2 μM).
SCH529074 purchased from MedChemExpress. Usage Cited in: Sci Rep. 2025 Aug 14;15(1):29794. [Abstract]
Annexin V-FITC/PI Double-staining apoptosis assay showing the percentage of apoptotic cell percentage of NP cells under p53 overexpression or SCH529074 (2 μM) treatment.
SCH529074 purchased from MedChemExpress. Usage Cited in: Sci Rep. 2025 Aug 14;15(1):29794. [Abstract]
The HE staining of the intervertebral disc treated with SCH529074.
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PLoS Comput Biol
2025 Mar 7;21(3):e1012847. PMID: 40053523 -
Solvant et solubilité
DMSO : 20 mg/mL (35.49 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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: ≥ 1 mg/mL (1.77 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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.
Pureté et documentation
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Fiche technique (278 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Miljana Nenkov, et al. Growth Inhibitory Role of the p53 Activator SCH 529074 in non‑small Cell Lung Cancer Cells Expressing Mutant p53. Oncol Rep. 2020 Jun;43(6):2073-2082. [Content Brief]
[2]. Mark Demma, et al. SCH529074, a Small Molecule Activator of Mutant p53, Which Binds p53 DNA Binding Domain (DBD), Restores Growth-Suppressive Function to Mutant p53 and Interrupts HDM2-mediated Ubiquitination of Wild Type p53. J Biol Chem. 2010 Apr 2;285( [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7744 mL | 8.8722 mL | 17.7443 mL | 44.3608 mL |
| 5 mM | 0.3549 mL | 1.7744 mL | 3.5489 mL | 8.8722 mL | |
| 10 mM | 0.1774 mL | 0.8872 mL | 1.7744 mL | 4.4361 mL | |
| 15 mM | 0.1183 mL | 0.5915 mL | 1.1830 mL | 2.9574 mL | |
| 20 mM | 0.0887 mL | 0.4436 mL | 0.8872 mL | 2.2180 mL | |
| 25 mM | 0.0710 mL | 0.3549 mL | 0.7098 mL | 1.7744 mL | |
| 30 mM | 0.0591 mL | 0.2957 mL | 0.5915 mL | 1.4787 mL |
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