2. Cell Cycle/DNA Damage Cytoskeleton Metabolic Enzyme/Protease Apoptosis Immunology/Inflammation NF-κB
  3. Microtubule/Tubulin MMP Bcl-2 Family Reactive Oxygen Species (ROS) Caspase
  4. Tubulin polymerization-IN-82

Tubulin polymerization-IN-82 is a tubulin inhibitor. Inhibits cell migration and invasion, and triggers cell apoptosis through the mitochondria and ER stress mediated pathway. Tubulin polymerization-IN-82 exhibits antitumor activity against drug resistance cancer cells, and inhibits tumor growth, can be used for liver cancer research.

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Tubulin polymerization-IN-82 Chemical Structure

Tubulin polymerization-IN-82 Chemical Structure

CAS No. : 3067075-77-5

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Tubulin polymerization-IN-82 Related Antibodies

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Description

Tubulin polymerization-IN-82 is a tubulin inhibitor. Inhibits cell migration and invasion, and triggers cell apoptosis through the mitochondria and ER stress mediated pathway. Tubulin polymerization-IN-82 exhibits antitumor activity against drug resistance cancer cells, and inhibits tumor growth, can be used for liver cancer research[1].

In Vitro

Tubulin polymerization-IN-82 (Compound 9n) (0.039-2.5 μM, 72 h) displays antiproliferative activities against different cells with IC50s of 0.09 μM (HepG-2), 0.25 μM (NCI-H460) , 0.20 μM (HCT-116) and 0.18 μM (SK-OV-3)[1].

Tubulin polymerization-IN-82 (0.039-2.5 μM, 72 h) has antiproliferative effect on drug-resistant cells with IC50s of 0.29 μM (A549/CDDP), 0.45 μM (A549/ Paclitaxel) and 0.51 μM (MCF-7/DOX)[1].

Tubulin polymerization-IN-82 (1.25-20 μM, 5-65 min) inhibits tubulin polymerization of purified tubulin, with an IC50 of 3.56 μM[1].

Tubulin polymerization-IN-82 (1.25 μM, 2.5 μM, 24 h) induces apoptosis of HepG-2 cells through a mitochondrial-mediated pathway and endoplasmic reticulum stress , disrupts the microtubule network in HepG-2 cells [1].

Tubulin polymerization-IN-82 (1.25 μM, 2.5 μM, 24 h) causes cell cycle arrest at the G2/M phase of HepG-2 cells in a concentration-dependent manner[1].

Tubulin polymerization-IN-82 (1.25 μM, 2.5 μM, 24 h) decreases the MMP of HepG-2 cells, induces ROS generation[1].

Tubulin polymerization-IN-82 (1.25 μM, 2.5 μM, 24 h) enhances intracellular Ca2+ levels and increases the expression levels of p-PERK, p-eIF2α, and CHOP in HepG-2 cells[1].

Tubulin polymerization-IN-82 (1.25 μM, 2.5 μM, 24 h) inhibits the cell colony formation, and inhibits cell migration and invasion of HepG-2 cells[1].

Tubulin polymerization-IN-82 was hydrolyzed by esterase after exposure to carboxylesterase for 4 h[1].

Tubulin polymerization-IN-82 remains stable at 24, 48 or 72 h under both PBS (pH = 7.4) and DMEM containing 1 % DMF[1].

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

Tubulin polymerization-IN-82 Related Antibodies

Apoptosis Analysis[1]

Cell Line: HepG-2 cells
Concentration: 1.25 and 2.5 μM
Incubation Time: 24 h
Result: Accounted for 13.76% and 31.2% of apoptotic cells (including early and late apoptotic cells). At the same concentration, apoptosis was induced more effectively by 9n (31.2%) than by CA-4 (20.18%).
Reduced the expression levels of cyclin B1, Cdc25c, and Cdc2 in HepG-2 cells.
Downregulated the expression of the anti-apoptotic protein Bcl-2 and upregulated the expression of the pro-apoptotic protein Bax in HepG-2 cells, activated the expression level of caspase-3 protein, triggered apoptosis in HepG-2 cells.

Cell Cycle Analysis[1]

Cell Line: HepG-2 cells
Concentration: 1.25 and 2.5 μM
Incubation Time: 24 h
Result: Caused cell cycle arrest at the G2/M phase.
Reduced expression levels of cyclin B1, Cdc25c, and Cdc2.
In Vivo

Tubulin polymerization-IN-82 (Compound 9n) (15 or 30 mg/kg, i.v., 21 days,) inhibits tumor growth in the HepG-2 xenograft model[1].

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

Animal Model: HepG-2 xenograft models in (Balb/c-nu) mice (6-week-old)[1].
Dosage: 15 or 30 mg/kg
Administration: i.v. ,for 21 days
Result: Inhibited tumor growth with the tumor growth inhibition (TGI) rates of 58.3% and 70.7%, respectively.
Not changed the body weight of the mice.
Not changed histopathology in the liver, heart, lung, spleen and kidney.
Molecular Weight

520.57

Formula

C30H32O8
CAS No.
SMILES

O=C(/C=C/C1=CC=C(OC)C=C1)OCCOC2=CC(/C=C\C3=CC(OC)=C(OC)C(OC)=C3)=CC=C2OC
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Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Tubulin polymerization-IN-82 Related Classifications

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Keywords:

Tubulin polymerization-IN-823067075-77-5Microtubule/TubulinMMPBcl-2 FamilyReactive Oxygen Species (ROS)CaspaseMatrix metalloproteinasesTubulin inhibitorpro-apoptosisanti-tumorA549/CDDPHepG-2HepG-2 xenograft modeldrug resistanceHepatocellular carcinomaHCCInhibitorinhibitorinhibit

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