Skp2-IN-4
Based on 1 Customer Validation
Skp2-IN-4 is an Skp2 inhibitor with a IC50 of 0.38 μM for Skp2-Cks1 binding. Skp2-IN-4 improves anti-tumor activity, inhibits the proliferation and induces S phase arrest by targeting Skp2. Skp2-IN-4 significantly enhances Cisplatin (HY-17394) chemosensitivity by suppressing the tumor cell stemness in NCl-H1299 xenograft mice model, promising for lung cancer and esophageal cancer research.
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- Pureté: 98.60%
- CAS No.: 3118494-67-7
- Formule: C24H19N5
- Masse moléculaire:377.44
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Skp2-IN-4 (Compound 10 h) potently inhibits tumor activity with IC50 s of 11.24 and 10.32 μM for lung cancer NCl-H1299 and esophageal cancer KYSE-510 cells, respectively[1].
Skp2-IN-4 (4 h) increases the protein's stability of Skp2 at the temperature range of 57-68 °C and disturbs the binding of Skp2 and Cks1 in KYSE-510 and NCl-H1299 cells[1].
Skp2-IN-4 (2.5-10 μM, 1-10 days) dose dependently inhibits cell colony formation and DNA synthesis in KYSE-510 and NCl-H1299 cells[1].
Skp2-IN-4 (5-15 μM, 48 h) dose dependently reduces the Skp2 expression, induces cellular accumulation of its substrates (p21 and p27) and arrests cell cycle at S phase with great efficacy at 10 μM in KYSE-510 and NCl-H1299 cells[1].
Skp2-IN-4 (10 μM, 48 h) significantly inhibits sphere formation and cell clonogenicity, induces G2/M phase cell cycle arrest and apoptosis, as well as suppressing the protein levels of CD44, Nanog, OCT4 and SOX2 (tumor stemness markers) with combination of Cisplatin in NCl-H1299 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:KYSE-510 cells, NCl-H1299 cells
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Concentration:5, 10, 15 μM
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Incubation Time:48 h
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Result:Significantly downregulated the expression of Skp2 in a dose-dependent manner in KYSE-510 and NCl-H1299 cells.
Increased the intracellular levels of p21 and p27 (substrates) in a dose-dependent manner in KYSE-510 and NCl-H1299 cells.
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Cell Line:KYSE-510 cells, NCl-H1299 cells
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Concentration:5, 10, 15 μM
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Incubation Time:48 h
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Result:Dose-dependently decreased the protein level of Skp2 but significantly increased the p21 and p27 expression in KYSE-510 and NCl-H1299 cells.
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Cell Line:KYSE-510 cells, NCl-H1299 cells
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Concentration:5, 10, 15 μM or 12.5 μg/mL Cisplatin
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Incubation Time:48 h
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Result:Induced a dose-dependent S phase arrest in KYSE-510 and NCl-H1299 cells.
Caused in a substantial cell cycle blockade with the S phase cell population from 17.51% to 41.92% in KYSE-510 cells as well as similar result in NCl-H1299 cells.
Significantly induced G2/M-phase cell cycle arrest at 10 μM with combination of Cisplatin in NCl-H1299 cells.
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Cell Line:KYSE-510 cells, NCl-H1299 cells
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Concentration:2, 5, 10 μM
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Incubation Time:7 days
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Result:Effectively inhibited cell colony formation in a concentration-dependently manner.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD-SCID mice (6 weeks old) were injected into the right axilla with NCl-H1299 cells (1 × 107 cells/mouse)[1].
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Dosage:25 mg/kg or Cisplatin (5 mg/kg)
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Administration:Oral gavage (p.o.), Cisplatin (i.p.), every 2 day for 20 days and then collected tumors and major organ tissues.
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Result:Significantly inhibited tumor growth, and reduced tumor volume and weight with combination of Cisplatin in NCl-H1299 xenograft mice model.
Induced no obvious toxicity with combination of Cisplatin in NCl-H1299 xenograft mice model.
Chemical Information
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CAS No. 3118494-67-7
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Appearance Solid
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Masse moléculaire 377.44
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Formule C24H19N5
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Color White to off-white
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SMILES
CN(CC1=CC=C(C#N)C=C1)C2=NC(C3=CC=CC=C3)=C(C4=CC=NC=C4)N=C2
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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
Solvant et solubilité
DMSO : 100 mg/mL (264.94 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: ≥ 2.5 mg/mL (6.62 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.
Pureté et documentation
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Fiche technique (277 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
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 | 2.6494 mL | 13.2471 mL | 26.4943 mL | 66.2357 mL |
| 5 mM | 0.5299 mL | 2.6494 mL | 5.2989 mL | 13.2471 mL | |
| 10 mM | 0.2649 mL | 1.3247 mL | 2.6494 mL | 6.6236 mL | |
| 15 mM | 0.1766 mL | 0.8831 mL | 1.7663 mL | 4.4157 mL | |
| 20 mM | 0.1325 mL | 0.6624 mL | 1.3247 mL | 3.3118 mL | |
| 25 mM | 0.1060 mL | 0.5299 mL | 1.0598 mL | 2.6494 mL | |
| 30 mM | 0.0883 mL | 0.4416 mL | 0.8831 mL | 2.2079 mL | |
| 40 mM | 0.0662 mL | 0.3312 mL | 0.6624 mL | 1.6559 mL | |
| 50 mM | 0.0530 mL | 0.2649 mL | 0.5299 mL | 1.3247 mL | |
| 60 mM | 0.0442 mL | 0.2208 mL | 0.4416 mL | 1.1039 mL | |
| 80 mM | 0.0331 mL | 0.1656 mL | 0.3312 mL | 0.8279 mL | |
| 100 mM | 0.0265 mL | 0.1325 mL | 0.2649 mL | 0.6624 mL |
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