SMU-G4
SMU-G4 is a Tubulin polymerization inhibitor. SMU-G4 induces G2/M phase cell cycle arrest, triggers Apoptosis, and upregulates the expression of Cleaved-Caspase 3. SMU-G4 exhibits in vivo anti-tumor activity in melanoma xenograft models. SMU-G4 can be used for research related to melanoma.
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- Formule: C20H19N3O3
- Masse moléculaire:349.38
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
[1]|
Caspase-3 |
In Vitro
SMU-G4 (multiple concentrations; 48 h) potently inhibits the proliferation of B16-F10, A549, and HepG2 cancer cells with IC50 values of 4 nM, 1.5 nM, and 44.8 nM, respectively[1].
SMU-G4 (1.5-3 μM) potently inhibits in vitro tubulin polymerization in a concentration-dependent manner, with near-complete suppression at 3 μM[1].
SMU-G4 (6.25-25 nM; 6 h) dose-dependently disrupts the microtubule network in HepG2 cells after 6 h of treatment[1].
SMU-G4 (6.25-12.5 nM; 24 h) induces concentration-dependent G2/M phase cell cycle arrest in B16-F10 cells, with 61.46% of cells in G2/M phase after 24 h treatment with 12.5 nM[1].
SMU-G4 (6.25-12.5 nM; 24 h) induces concentration-dependent apoptosis in B16-F10 cells, with 18.90% of cells apoptotic after 24 h treatment with 12.5 nM[1].
SMU-G4 (1-12 nM; 24 h) dose-dependently increases Cleaved-Caspase 3 expression in B16-F10 cells after 24 h of treatment[1].
SMU-G4 (6.25-25 nM; 24 h) dose-dependently inhibits B16-F10 cell migration, achieving a 70.78% inhibition rate after 24 h treatment with 25 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:B16-F10 mouse melanoma cells, A549 human non-small cell lung cancer cells, HepG2 human hepatocellular carcinoma cells
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Concentration:multiple concentrations
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Incubation Time:48 h
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Result:Potently inhibited proliferation of B16-F10 cells with an IC50 of 4 nM.
Potently inhibited proliferation of A549 cells with an IC50 of 1.5 nM.
Potently inhibited proliferation of HepG2 cells with an IC50 of 44.8 nM.
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Cell Line:HepG2 human hepatocellular carcinoma cells
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Concentration:6.25 nM, 12.5 nM, 25 nM
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Incubation Time:6 h
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Result:Induced a progressive, dose-dependent collapse of the HepG2 cell microtubule network, phenocopying the effects of CA-4 and colchicine.
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Cell Line:B16-F10 mouse melanoma cells
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Concentration:6.25 nM, 12.5 nM
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Incubation Time:24 h
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Result:Increased the percentage of B16-F10 cells in G2/M phase from 4.67% (control) to 29.96% at 6.25 nM.
Increased the percentage of B16-F10 cells in G2/M phase to 61.46% at 12.5 nM, which was comparable to CA-4 at 6.25 nM (63.44%) and far superior to colchicine at 25 nM (11.21%).
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Cell Line:B16-F10 mouse melanoma cells
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Concentration:6.25 nM, 12.5 nM
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Incubation Time:24 h
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Result:Increased the total percentage of apoptotic B16-F10 cells from 2.94% (control) to 14.38% at 6.25 nM.
Increased the total percentage of apoptotic B16-F10 cells to 18.90% at 12.5 nM.
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Cell Line:B16-F10 mouse melanoma cells
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Concentration:1 nM, 3 nM, 6 nM, 12 nM
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Incubation Time:24 h
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Result:Induced a dose-dependent increase in Cleaved-Caspase 3 levels in B16-F10 cells.
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Cell Line:B16-F10 mouse melanoma cells
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Concentration:6.25 nM, 12.5 nM, 25 nM
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Incubation Time:24 h
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Result:Inhibited B16-F10 cell migration with an inhibition rate of 31.95% at 6.25 nM.
Inhibited B16-F10 cell migration with an inhibition rate of 61.88% at 12.5 nM, which was comparable to CA-4 at 12.5 nM (62.53%) and substantially more effective than colchicine at 12.5 nM (15.77%).
Inhibited B16-F10 cell migration with an inhibition rate of 70.78% at 25 nM.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (female, 5 weeks old, subcutaneous implantation of 4×105 B16-F10 cells)[1]
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Dosage:15 mg/kg; 30 mg/kg
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Administration:daily; 10 days
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Result:Achieved a tumor growth inhibition (TGI) value of 74.4% at 15 mg/kg.
Increased TGI to 81.91% at 30 mg/kg.
Recorded no significant body weight loss or observable signs of toxicity over the 10-day period.
- RNA extraction experimental
- Annexin V plus membrane-impermeant dye apoptosis staining
- BrdU Incorporation Assay
- Protocol for Cell Cycle
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Flow cytometric DNA-content cell-cycle staining
- Patient-Derived Xenograft (PDX)
- Apoptosis Solutions
- Splenic/Portal-Vein Liver Metastasis Xenograft
- Subcutaneous Cell-Line-Derived Xenograft
- Orthotopic Cell-Line Xenograft
- Intraperitoneal/Peritoneal Dissemination Xenograft
Chemical Information
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Masse moléculaire 349.38
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Formule C20H19N3O3
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SMILES
CN(N=C1C#N)C(C1=C2)=CC=C2/C=C\C3=CC(OC)=C(OC)C(OC)=C3
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
SMU-G4 Related Classifications
HY-183790 Related Classifications
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