Art. -Nr.: HY-110088

SCH529074

3 Cited Publications

Kundenbewertung

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 K_i 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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Reinheit: 99.73%
CAS. Nr.: 922150-11-6
Formel: C₃₁H₃₆Cl₂N₆
Molecular Weight:563.56

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

SCH529074 Chemical Structure

CAS. Nr.: 922150-11-6

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (3)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

Ki: 1-2 μM (p53 DBD)^[2]

In Vitro

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.

Cell Viability Assay^[1]

Cell Line:

p53 mutant cells (H157, H1975 and H322) and p53 WT cell line A549
Concentration:

2 µM; 4 µM
Incubation Time:

24 hours
Result:

Inhibited cancer WT and mutant cell viability.

Cell Cycle Analysis^[1]

Cell Line:

H1975, H157, A549, HCT116, HCT116 p53^-/- cells
Concentration:

2 µM, 4 µM, 6 µM
Incubation Time:

24 hours
Result:

Induced apoptosis in all assessed NSCLC cell lines irrespective of their p53 mutational status.

Western Blot Analysis^[1]

Cell Line:

H1975, H322, H157, A549, HCT116, HCT116 p53^-/-
Concentration:

2 µM, 4 µM, 6 µM
Incubation Time:

24 hours
Result:

Increased PUMA and p21 protein expression.

In Vivo

SCH529074 (oral administration; 30 or 50 mg/kg; twice daily; 4 weeks; started on day 3 until day 31) causes 79 and 43% reduction of tumor growth at 50 and 30 mg/kg doses, respectively. the degree of tumor inhibition correlates with the plasma exposure of the compound (0.26–0.55 μm?at 30 mg/kg and 0.39-0.79 μm?at 50 mg/kg, 2-12 h post final dosing) in human DLD-1 colorectal cancer xenograft^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Female nude mice, 5–7 weeks of age, received subcutaneous inoculation of DLD-1 human colorectal carcinoma cells^[2]
Dosage:

30 or 50 mg/kg
Administration:

Oral administration; twice daily; 4 weeks; started on day 3 until day 31
Result:

Inhibited tumor growth

Chemical Information

CAS. Nr. 922150-11-6
Appearance Solid
Molecular Weight 563.56
Formel C₃₁H₃₆Cl₂N₆
Color Off-white to light yellow
SMILES

CN(C)CCCNC1=C2C=CC=CC2=NC(CN3CCN(C(C4=CC=C(Cl)C=C4)C5=CC=C(Cl)C=C5)CC3)=N1
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (3)

All RT-PCRWBCell Migration/Invasion AssayFlow CytometryHistological Imaging/Staining

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Journal Impact Factor

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.
PLoS Comput Biol

iSoMAs: Finding isoform expression and somatic mutation associations in human cancers. [Abstract]

2025 Mar 7;21(3):e1012847. PMID: 40053523
bioRxiv

2023 Jul 7.

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.7744 mL

8.8722 mL

17.7443 mL

5 mM

0.3549 mL

1.7744 mL

3.5489 mL

10 mM

0.1774 mL

0.8872 mL

1.7744 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 1 mg/mL (1.77 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

SCH529074

3 Cited Publications

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SCH529074

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Orally Active Compound Library

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Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

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Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Apoptosis Compound Library

Anti-Cancer Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Publications Citing Use of MedChemExpress (MCE) SCH529074

Biologische Aktivität

Chemical Information

Publications (3)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

SCH529074

Ferroptosis Compound Library

Pyroptosis Compound Library

Orally Active Compound Library

Glutamine Metabolism Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Transcription Factor-Targeted Library

Anti-Colorectal Cancer Compound Library

Heterocyclic Compound Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Apoptosis Compound Library

Anti-Cancer Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Publications Citing Use of MedChemExpress (MCE) SCH529074

Biologische Aktivität

Chemical Information

Publications (3)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

SCH529074 Related Classifications

HY-110088 Related Classifications