2. Metabolic Enzyme/Protease
  3. E1/E2/E3 Enzyme
  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.

For research use only. We do not sell to patients.

Skp2-IN-4 Chemical Structure

Skp2-IN-4 Chemical Structure

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Skp2-IN-4 Related Antibodies

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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
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

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
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Skp2-IN-4 Related Classifications

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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 EnzymeE1 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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