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Art. -Nr.: HY-182752

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CDK1-IN-9

CDK1-IN-9 is an orally active and selective CDK1 inhibitor with an IC₅₀ of 5.5 nM. CDK1-IN-9 exhibits broad antiproliferative activity, particularly against HCT116 colon cancer cells. CDK1-IN-9 induces G2/M phase arrest and downregulates CDK1, cyclin B1, and the replication initiation factor CDC45. CDK1-IN-9 induces severe DNA replication stress, subsequently activating the p53 signaling pathway to trigger apoptosis. CDK1-IN-9 can be used for research on colon cancer, liver cancer and gastric cancer.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Formel: C₁₆H₁₇N₇O₃S₂
Molecular Weight:419.48

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

CDK1-IN-9 Chemical Structure

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Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

CDK1/cyclinB1

5.5 nM (IC₅₀)

CDK2/cyclinE

25.9 nM (IC₅₀)

CDK4/cyclin D

402.8 nM (IC₅₀)

Aurora A

77.8 nM (IC₅₀)

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In Vitro

CDK1-IN-9 (compound 11I) (0.1-5 μM; 24-72 h) exhibits IC₅₀s of 0.023 μM, 0.292 μM, 0.360 μM and 0.566 μM in HCT116 cell line, HepG2 cell line, SGC7901 cell line and normal keratinocyte line HaCaT, respectively^[1].
CDK1-IN-9 (0.1-0.5 μM; 3 days) strongly suppresses the clonogenic survival of HCT116 cell line, HepG2 cell line and SGC7901 cell line, respectively^[1].
CDK1-IN-9 (0.5 μM; 24-48 h) significantly impairs the migratory ability of HCT116 cells^[1].
CDK1-IN-9 (0.01-0.1 μM; 72 h) induces G2/M arrest in the HCT116 cell line^[1].
CDK1-IN-9 (0.1-0.5 μM; 72 h) induces G2/M arrest in HepG2 and SGC7901 cell lines^[1].
CDK1-IN-9 (0.1-1 μM; 72 h) inhibits the CDK1/cyclin B1 kinase activity through a non-canonical pathway^[1].
CDK1-IN-9 (1 μM; 72 h) inhibits cell division cycle protein 45 (CDC45) activity, causes DNA damage, and triggers apoptosis via the p53-mediated mitochondrial pathway, which can be reproduced by CDC45 knockdown in the HCT116 cell line^[1].

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

Cell Viability Assay^[1]

Cell Line:

HCT116 cell line, HepG2 cell line, SGC7901 cell line
Concentration:

0.1 μM; 0.25 μM; 0.5 μM; 1 μM; 2.5 μM; 5 μM
Incubation Time:

24 h; 48 h; 72 h
Result:

Decreased the viability of HCT116, HepG2, and SGC7901 cells in a dose- and time-dependent manner.

Cell Migration Assay ^[1]

Cell Line:

HCT116 cell line
Concentration:

0.5 μM
Incubation Time:

24 h; 48 h
Result:

Significantly impaired the migratory ability.

Cell Cycle Analysis^[1]

Cell Line:

HepG2 cell line, SGC7901 cell line
Concentration:

0.1 μM; 0.5 μM
Incubation Time:

72 h
Result:

Induced G2/M arrest in a concentration-dependent manner.

Cell Cycle Analysis^[1]

Cell Line:

HCT116 cell line
Concentration:

0.01 μM; 0.1 μM
Incubation Time:

72 h
Result:

Induced G2/M arrest in a concentration-dependent manner.

Apoptosis Analysis^[1]

Cell Line:

HCT116 cell line, HepG2 cell line, SGC7901 cell line
Concentration:

0.01 μM; 0.1 μM; 0.5 μM
Incubation Time:

72 h
Result:

Induced apoptosis in a concentration-dependent manner.

Western Blot Analysis^[1]

Cell Line:

HCT116 cell line
Concentration:

0.1 μM; 0.5 μM; 1 μM
Incubation Time:

72 h
Result:

Reduced the protein levels of CDK1 and cyclin B1 in a concentration-dependent fashion.
Significantly reduced CDC45 expression.
Increased γH2AX accumulation.
Elevated both total and phosphorylated levels of p53.
Decreased the ratio of the anti-apoptotic protein Bcl-xL to the pro-apoptotic protein BAX.
Increased Cytochrome c release.

Real Time qPCR^[1]

Cell Line:

HCT116 cell line
Concentration:

0.5 μM; 1 μM
Incubation Time:

24 h; 48 h; 72 h
Result:

Downregulated the transcriptional levels of CDK1 and cyclin B1.

In Vivo

CDK1-IN-9 (3.3-30 mg/kg; i.g.; every day; for 14 days) markedly suppressed xenograft tumor growth in male BALB/c nude mice, without inducing significant body weight loss or observable organ toxicity^[1].

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

Animal Model:

Male BALB/c nude mice (4-6 weeks old; 16-20 g) received a subcutaneous injection of 1 × 10⁷ HCT116 cells to establish a xenograft tumor model^[1].
Dosage:

3.3 mg/kg; 10 mg/kg; 30 mg/kg
Administration:

i.g.; every day; for 14 days
Result:

Significantly lower tumor volume compared with the control group.
Reduced tumor weight by 56.4% in 30 mg/kg group.
Did not have significant changes in mouse body weight or in the weights of major organs (heart, liver, spleen, lung, and kidney).
Showed no obvious pathological injury or toxicity in these tissues through histological examination.
Did not have significantly effect on serum biochemistry parameters (including ALT and AST).

Chemical Information

Molecular Weight 419.48
Formel C₁₆H₁₇N₇O₃S₂
SMILES

S=C(N1N=C(NC2=CC=C(S(=O)(N)=O)C=C2)N=C1N)NC3=CC=CC=C3OC
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Wu L, et al. Design and synthesis of novel 1,2,4-triazolobenzene sulfonamide derivatives as selective CDK1 inhibitors with potent in vivo anticancer efficacy. Eur J Med Chem. 2026 Jun 5;310:118799. [Content Brief]

Calculators

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)}

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.

Keywords

100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise

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CDK1-IN-9

Alle CDK Isoform-spezifische Produkte anzeigen

Alle Aurora Kinase Isoform-spezifische Produkte anzeigen