1. Cell Cycle/DNA Damage Cytoskeleton Apoptosis
  2. Microtubule/Tubulin Apoptosis
  3. Tubulin polymerization-IN-5

Tubulin polymerization-IN-5 (compound 20q) is a potent tubulin inhibitor with potential anticancer activities. Tubulin polymerization-IN-5 can arrest ESCC cells at G2/M phase and cause cells apoptosis.

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Tubulin polymerization-IN-5 Chemical Structure

Tubulin polymerization-IN-5 Chemical Structure

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Description

Tubulin polymerization-IN-5 (compound 20q) is a potent tubulin inhibitor with potential anticancer activities. Tubulin polymerization-IN-5 can arrest ESCC cells at G2/M phase and cause cells apoptosis[1].

IC50 & Target

Tubulin

In Vitro

Tubulin polymerization-IN-5 (compound 20q) (0-100 nM, 48 h) exhibits potent antiproliferative activity against Kyse30, Kyse450, MGC-803, and HCT-116 cells[1].
Tubulin polymerization-IN-5 (0-60 nM, 7 d) obviously inhibits the cellular colony formation ability of the Kyse30 and Kyse450 cells[1].
Tubulin polymerization-IN-5 (0-100 nM, 48 h) inhibits microtubule assembly and disrupts cytoskeleton[1].
Tubulin polymerization-IN-5 (0-300 nM, 24 h) causes a significant weakening of the β-tubulin adduct band in Kyse30 and Kyse450 cells, competitively bind the colchicine binding site of β-tubulin[1].
Tubulin polymerization-IN-5 (0-100 nM, 48 h) effectively arrests cells at the G2/M phase, and induces cell apoptosis in Kyse30 and Kyse450 cells by regulating the expression of related proteins[1].
Tubulin polymerization-IN-5 (0-100 nM, 48 h) induces cell mitochondrial apoptosis in ESCC cells, leads to a significant depolarization of mitochondria membrane potential in Kyse30 and Kyse450 cells[1].

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

Cell Proliferation Assay

Cell Line: Kyse30, Kyse450, MGC-803, and HCT-116 cells[1]
Concentration: 0, 80, 100 nM
Incubation Time: 48 h
Result: Exhibited potent antiproliferative activity against Kyse30, Kyse450, MGC-803, and HCT-116 cells, with IC50 values of 0.069, 0.078, 0.084, and 0.227 μM, respectively.

Cell Cycle Analysis

Cell Line: Kyse30 and Kyse450 cells[1]
Concentration: 0, 80, 100 nM
Incubation Time: 48 h
Result: Effectively arrested 2 ESCC cells at the G2/M phase, significantly increased of percentages of cells at the G2/M phase from 19.38 to 76.9767 in Kyse30 cells, and 7.04333 to 80.8933 in Kyse450 cells.

Apoptosis Analysis

Cell Line: Kyse30 and Kyse450 cells[1]
Concentration: 0, 80, 100 nM
Incubation Time: 48 h
Result: Dose-dependently induced cell apoptosis in Kyse30 and Kyse450 cells, significantly increased the percentages of total apoptotic cells from 8.1667% (0 nM) to 23.8% (80 nM, Kyse30 cells), 34.0333% (80 nM, Kyse450 cells), 38.633% (100 nM, Kyse30 cells), and 57.3667% (100 nM, Kyse450 cells), respectively.

Western Blot Analysis

Cell Line: Kyse30 and Kyse450 cells[1]
Concentration: 0, 80, 100 nM
Incubation Time: 48 h
Result: Dose-dependently down-regulated the expression of the G2 phase related proteins CDK1, CDC25c and p-Wee 1, up-regulated the level of the M phase marker protein p-Histone H3; up-regulated the activity of the executors of apoptosis caspase-3, up-regulated the pro-apoptotic proteins Bax and Noxa, and down-regulated the anti-apoptotic protein Bcl-2, decreased the levels of IAP (Inhibitor of Apoptosis Proteins) family protein XIAP.
Molecular Weight

621.77

Formula

C29H39N3O8S2

SMILES

COC1=CC(N(C(CSC(N2CCN(CC2)C(OC(C)(C)C)=O)=S)=O)CC3=CC(O)=C(C=C3)OC)=CC(OC)=C1OC

Shipping

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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Help & FAQs
  • 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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Tubulin polymerization-IN-5
Cat. No.:
HY-144299
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