Art. -Nr.: HY-174346

Skp2-IN-4

Kundenbewertung

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.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 98.60%
CAS. Nr.: 3118494-67-7
Formel: C₂₄H₁₉N₅
Molecular Weight:377.44

Speicherung:

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

Skp2-IN-4 Chemical Structure

CAS. Nr.: 3118494-67-7

Größe

Preis

Verfügbarkeit

Menge

Amount: USD 0.00

* Bitte wählen Sie Menge, bevor Sie Artikel hinzufügen.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen :

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.

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.

Chemical Information

CAS. Nr. 3118494-67-7
Appearance Solid
Molecular Weight 377.44
Formel C₂₄H₁₉N₅
Color White to off-white
SMILES

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

Lösungsmittel & Löslichkeit

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)

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

2.6494 mL

13.2471 mL

26.4943 mL

5 mM

0.5299 mL

2.6494 mL

5.2989 mL

10 mM

0.2649 mL

1.3247 mL

2.6494 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: ≥ 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.

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:

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 (277 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]. Hu K, et al. Molecular hybridization strategy - discovery of 2,3-diarylpyrazine derivatives as potent Skp2 inhibitors with improved anti-tumor activity and enhanced cisplatin sensitivity. Eur J Med Chem. 2025 Oct 5; 295:117788. [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	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

Keywords

Produktname:
Art. -Nr.:
Menge:
MCE Japan Authorized Agent:

Produktname:
CAS. Nr.:
Species:
Reinheit:
Menge:

Skp2-IN-4

MCE Bioactive Compound Library

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Skp2-IN-4 Related Classifications

Art. -Nr.: HY-174346