Tubulin-IN-53
Tubulin-IN-53 is a potent Tubulin inhibitor with an IC50 of 6.06 μM. Tubulin-IN-53 inhibits the polymerization of tubulin by targeting the colchicine binding site of tubulin and destroys the microtubule network. Tubulin-IN-53 induces MCF-7 cell cycle arrest in the G2/M phase and apoptosis, and inhibits cell migration accompanied by the decrease of mitochondrial membrane potential and increase the accumulation of ROS. Tubulin-IN-53 destroys the angiogenesis of human umbilical vein endothelial cells.Tubulin-IN-53 can used for the study of cancers such as breast cancer and lung cancer.
For research use only. We do not sell to patients.
- Formula: C20H16ClNO6
- Molecular Weight:401.80
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
In Vitro
Tubulin-IN-53 (Compound A7) (72 h) exhibits antiproliferative activities in various cancer cells with IC50s of 6, 4, 5, 6, 4 and 10 nM against PC-3, MCF-7, MDA-MB-231, A549, HT-29 and A549/TxR cells and cytotoxicity on normal cells with CC50s of 112 and 220 nM against L02 and MCF-10A cells[1].
Tubulin-IN-53 (5-20 nM, 14 d) consistently inhibits MCF-7 cells colony formation[1].
Tubulin-IN-53 (5-20 nM, 6 h) dose-dependently inhibits the the formation of EBI and β-tubulin adducts and completely disaggregats the microtubule network in MCF-7 cells[1].
Tubulin-IN-53 (5-20 nM, 24 h) induces MCF-7 cell cycle arrest in the G2/M phase and cell apoptosis, and significantly increases intracellular ROS levels[1].
Tubulin-IN-53 (2.5-10 nM, 24 h) inhibits A549 cell migration and effectively inhibits the formation of vascular networks in HUVECs[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF-7 cells
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Concentration:5, 10 and 20 nM
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Incubation Time:24 h
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Result:Significantly increased apoptosis rate.
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Cell Line:MCF-7 cells
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Concentration:5, 10 and 20 nM
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Incubation Time:24 h
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Result:Increased the G2/M phase ratio of MCF-7 cells from 18.7% to 76.1%.
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Cell Line:MCF-7 cells
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Concentration:5, 10 and 20 nM
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Incubation Time:24 h
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Result:Upregulated Cyclin B1 expression and reduced Cdc2 phosphorylation (Y15) levels.
Downregulates the anti-apoptotic protein Bcl-2 and upregulates the pro-apoptotic protein Bax.
Increased cleaved PARP and cleaved caspase-3 levels.
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Cell Line:A549 cells
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Concentration:2.5, 5 and 10 nM
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Incubation Time:24 h
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Result:Significantly reduced the number of A549 cells penetrating the membrane.
Significantly inhibited the migration ability of A549 cells.
- Human pluripotent stem cell endothelial-cell differentiation
- Cell migration
- Breast Cancer Modeling
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Flow cytometric DNA-content cell-cycle staining
- Zigmond Chamber Chemotaxis Assay
- Under-Agarose Cell Migration Assay
- Transwell/Boyden Chamber Migration Assay
- Fluorescent plasma-membrane potential dye assay
- Mitochondrial membrane-potential and mitochondrial mass staining
- Endothelial Tube Formation Assay
- Apoptosis Solutions
- 3D Collagen/Hydrogel Matrix Migration Assay
- Cell-Exclusion Zone Migration Assay
- Dunn/Insall Chamber Chemotaxis Assay
- Endothelial Cell Migration/Angiogenic Sprouting Assay
- Scratch/Wound-Healing Migration Assay
- Mitochondrial membrane-potential fluorescent assay
- Vascular/Branching Fractal Analysis
- Annexin V plus membrane-impermeant dye apoptosis staining
- BrdU Incorporation Assay
- ROS/oxidative-stress fluorescent staining
- Neural Crest/Neuronal Cell Migration Explant Assay
- Protocol for Cell Cycle
Chemical Information
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Molecular Weight 401.80
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Formula C20H16ClNO6
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SMILES
O=C1OCC2=C1C(C3=CC(OC)=C(OC)C(Cl)=C3)C4=CC5=C(OCO5)C=C4N2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)