2. Metabolic Enzyme/Protease Apoptosis Cell Cycle/DNA Damage
  3. E1/E2/E3 Enzyme Apoptosis DNA/RNA Synthesis
  4. Skp2-IN-4

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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Skp2-IN-4

Skp2-IN-4 Chemical Structure

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Based on 1 publication(s) in Google Scholar

Skp2-IN-4 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

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Description

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[1].

In Vitro

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.

Skp2-IN-4 Related Antibodies

Immunofluorescence[1]

Cell Line: KYSE-510 cells, NCl-H1299 cells
Concentration: 5, 10, 15 μM
Incubation Time: 48 h
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.

Western Blot Analysis[1]

Cell Line: KYSE-510 cells, NCl-H1299 cells
Concentration: 5, 10, 15 μM
Incubation Time: 48 h
Result: Dose-dependently decreased the protein level of Skp2 but significantly increased the p21 and p27 expression in KYSE-510 and NCl-H1299 cells.

Cell Cycle Analysis[1]

Cell Line: KYSE-510 cells, NCl-H1299 cells
Concentration: 5, 10, 15 μM or 12.5 μg/mL Cisplatin
Incubation Time: 48 h
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.

Cell Proliferation Assay[1]

Cell Line: KYSE-510 cells, NCl-H1299 cells
Concentration: 2, 5, 10 μM
Incubation Time: 7 days
Result: Effectively inhibited cell colony formation in a concentration-dependently manner.
In Vivo

Skp2-IN-4 (Compound 10 h) (25  mg/kg, p.o., every 2 day for 20 days) increases the chemosensitivity of NCl-H1299 cells to Cisplatin and potently inhibits tumor growth in the NCl-H1299 xenograft mice model[1].

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

Animal Model: NOD-SCID mice (6 weeks old) were injected into the right axilla with NCl-H1299 cells (1 × 107 cells/mouse)[1].
Dosage: 25  mg/kg or Cisplatin (5 mg/kg)
Administration: Oral gavage (p.o.), Cisplatin (i.p.), every 2 day for 20 days and then collected tumors and major organ tissues.
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.
Molecular Weight

377.44

Formula

C24H19N5
Appearance

Solid

SMILES

CN(CC1=CC=C(C#N)C=C1)C2=NC(C3=CC=CC=C3)=C(C4=CC=NC=C4)N=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6494 mL 13.2471 mL 26.4943 mL
5 mM 0.5299 mL 2.6494 mL 5.2989 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

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

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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

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In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

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

    Solubility: ≥ 2.5 mg/mL (6.62 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
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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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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
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 2.6494 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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Skp2-IN-4 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Skp2-IN-4E1/E2/E3 EnzymeApoptosisDNA/RNA SynthesisE1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligaseS-phase kinase-associated protein 2Skp2ChemosensitivityNCl-H1299 cellsKYSE-510 cellsNCl-H1299 xenograft mice modelInhibitorinhibitorinhibit

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