Skp2 inhibitor 3
Based on 1 Customer Validation
Skp2 inhibitor 3 is an orally active inhibitor of the Skp2-Cks1 complex, with an IC50 of 4.86 μM. Skp2 inhibitor 3 reduces Skp2 protein expression while upregulating the expression of p21 and p27. Skp2 inhibitor 3 inhibits colony formation and migration of cancer cells, and induces cell cycle arrest at the S phase. Skp2 inhibitor 3 suppresses tumor growth in xenograft mice. Skp2 inhibitor 3 can be used in the research of gastric cancer and prostate cancer.
For research use only. We do not sell to patients.
- Purity: 98.07%
- CAS No.: 3098980-02-7
- Formula: C21H19BrN4O2S
- Molecular Weight:471.37
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Metabolism/Protease Compound Library
HY-L012
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Anti-Cancer Compound Library
HY-L025
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Oxygen Sensing Compound Library
HY-L045
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Ubiquitination Compound Library
HY-L050
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Orally Active Compound Library
HY-L061
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Anti-Liver Cancer Compound Library
HY-L101
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Anti-Prostate Cancer Compound Library
HY-L124
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Bioactive Compound Library Max
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Bioactive Compound Library
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Anti-Gastric Cancer Compound Library
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Amino Acid Metabolism Compound Library
HY-L189
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Cell Proliferation Compound Library
HY-L201
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High-Throughput Bioactive Compound Library
HY-L205
Biological Activity
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Skp2 4.86 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MGC-803 | IC50 |
10.85 μM
Compound: E35
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Inhibition of cell proliferation in human MGC-803 cells incubated for 72 hrs by MTT assay
Inhibition of cell proliferation in human MGC-803 cells incubated for 72 hrs by MTT assay
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[PMID: 39285177] |
| PC-3 | IC50 |
11.74 μM
Compound: E35
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Inhibition of cell proliferation in human PC-3 cells incubated for 72 hrs by MTT assay
Inhibition of cell proliferation in human PC-3 cells incubated for 72 hrs by MTT assay
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[PMID: 39285177] |
Skp2 inhibitor 3 (Compound E35) (2.0-50 μM; 24-72 h) inhibits the proliferation of MGC-803 and PC-3 cells in a time- and dose-dependent manner, with IC50 values of 10.85 μM and 11.74 μM, respectively[1].
Skp2 inhibitor 3 (1.0-3.0 μM; 10 days) dose-dependently inhibits colony formation of MGC-803 and PC-3 cells, with nearly complete inhibition observed at 3.0 μM[1].
Skp2 inhibitor 3 (2.5-7.5 μM; 26 h) inhibits DNA synthesis in MGC-803 and PC-3 cells in a dose-dependent manner[1].
Skp2 inhibitor 3 (2.5-7.5 μM; 48 h) dose-dependently inhibits the migration of MGC-803 and PC-3 cells in wound healing assays[1].
Skp2 inhibitor 3 (1.0-3.0 μM; 36 h) inhibits the invasion of MGC-803 and PC-3 cells in a dose-dependent manner in Transwell assays[1].
Skp2 inhibitor 3 (5.0-15.0 μM; 6-48 h) induces S-phase cell cycle arrest in MGC-803 and PC-3 cells in a concentration-dependent manner[1].
Skp2 inhibitor 3 (5.0-15.0 μM; 6-48 h) reduces Skp2 protein expression in a dose- and time-dependent manner in MGC-803 and PC-3 cells, while upregulating the expression of its substrates p21 and p27[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MGC-803 gastric cancer cells, PC-3 prostate cancer cells
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Concentration:2.0, 3.5, 6.5, 13, 25 and 50 μM
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Incubation Time:24 h, 48 h, 72 h
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Result:Inhibited cell viability in a time-dependent and dose-dependent manner.
Exhibited IC50 values of 10.85 μM in MGC-803 cells and 11.74 μM in PC-3 cells.
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Cell Line:MGC-803 gastric cancer cells, PC-3 prostate cancer cells
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Concentration:2.5, 5.0 and 7.5 μM
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Incubation Time:48 h
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Result:Significantly reduced wound closure in a dose-dependent manner, with wound closure rates decreasing with increasing compound concentration in both cell lines.
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Cell Line:MGC-803 gastric cancer cells, PC-3 prostate cancer cells
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Concentration:1.0, 2.0 and 3.0 μM
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Incubation Time:36 h
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Result:Significantly reduced the number of invaded cells in a dose-dependent manner, with highly significant decreases at 2.0 and 3.0 μM compared to controls in both cell lines.
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Cell Line:MGC-803 gastric cancer cells, PC-3 prostate cancer cells
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Concentration:5.0, 7.5 and 15.0 μM
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Incubation Time:36 h (concentration-dependent); 6, 12, 24, 36, 48 h (time-dependent)
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Result:Increased the percentage of MGC-803 cells in S-phase from 22.8% to 45.1% and PC-3 cells in S-phase from 18.2% to 44.3% at 15.0 μM for 36 h.
Gradually increased the percentage of S-phase cells in both lines over 36 h with 15.0 μM treatment; at 48 h, S-phase percentage decreased and G2/M percentage increased, likely due to increased cell death.
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Cell Line:MGC-803 gastric cancer cells, PC-3 prostate cancer cells
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Concentration:5.0, 7.5 and 15.0 μM
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Incubation Time:48 h (concentration-dependent); 6, 12, 24, 36, 48 h (time-dependent)
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Result:Decreased Skp2 protein levels in a dose-dependent manner, while increasing p21 and p27 protein levels correspondingly in both cell lines.
Decreased Skp2 protein levels over time, while p21 and p27 protein levels gradually increased over 48 h in both cell lines.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD-SCID (6-week-old)[1]
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Dosage:25 mg/kg; 50 mg/kg
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Administration:p.o.; once every 2 days; 21 days
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Result:Achieved a tumor growth inhibitory rate of 50.9% at 25 mg/kg.
Achieved a tumor growth inhibitory rate of 76.9% at 50 mg/kg.
Caused no significant changes in mouse body weight.
Showed no obvious morphological differences in major organs (heart, liver, spleen, lung, kidney) between treated and vehicle groups via H&E staining.
Chemical Information
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CAS No. 3098980-02-7
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Appearance Solid
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Molecular Weight 471.37
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Formula C21H19BrN4O2S
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Color White to off-white
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SMILES
COC1=CC=C(C2=CC(C)=NC3=NC(SCC4=CC=C(Br)C=C4)=NN32)C(OC)=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 10 mg/mL (21.21 mM; ultrasonic and warming and heat to 60°C; 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.
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.
Purity & Documentation
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Data Sheet (279 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)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
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 | 2.1215 mL | 10.6074 mL | 21.2148 mL | 53.0369 mL |
| 5 mM | 0.4243 mL | 2.1215 mL | 4.2430 mL | 10.6074 mL | |
| 10 mM | 0.2121 mL | 1.0607 mL | 2.1215 mL | 5.3037 mL | |
| 15 mM | 0.1414 mL | 0.7072 mL | 1.4143 mL | 3.5358 mL | |
| 20 mM | 0.1061 mL | 0.5304 mL | 1.0607 mL | 2.6518 mL |
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