1. Cell Cycle/DNA Damage Cytoskeleton Apoptosis Immunology/Inflammation NF-κB Metabolic Enzyme/Protease
  2. Microtubule/Tubulin Apoptosis Reactive Oxygen Species (ROS)
  3. 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.

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Tubulin-IN-53

Tubulin-IN-53 Chemical Structure

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Description

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[1].

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.

Apoptosis Analysis[1]

Cell Line: MCF-7 cells
Concentration: 5, 10 and 20 nM
Incubation Time: 24 h
Result: Significantly increased apoptosis rate.

Cell Cycle Analysis[1]

Cell Line: MCF-7 cells
Concentration: 5, 10 and 20 nM
Incubation Time: 24 h
Result: Increased the G2/M phase ratio of MCF-7 cells from 18.7% to 76.1%.

Western Blot Analysis[1]

Cell Line: MCF-7 cells
Concentration: 5, 10 and 20 nM
Incubation Time: 24 h
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.

Cell Migration Assay [1]

Cell Line: A549 cells
Concentration: 2.5, 5 and 10 nM
Incubation Time: 24 h
Result: Significantly reduced the number of A549 cells penetrating the membrane.
Significantly inhibited the migration ability of A549 cells.
Molecular Weight

401.80

Formula

C20H16ClNO6

SMILES

O=C1OCC2=C1C(C3=CC(OC)=C(OC)C(Cl)=C3)C4=CC5=C(OCO5)C=C4N2

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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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  • 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.

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Product Name:
Tubulin-IN-53
Cat. No.:
HY-175512
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