2. Cytoskeleton Cell Cycle/DNA Damage Apoptosis
  3. Microtubule/Tubulin Apoptosis
  4. Tubulin polymerization-IN-28

Tubulin polymerization-IN-28 (compound-4) is a microtubule protein polymerization inhibitor with highly selective anticancer activity. Tubulin polymerization-IN-28 can be activated by NQO1 and effectively release combretastatin A-4 to kill tumor cells. Tubulin polymerization-IN-28 can induce cell apoptosis and be used in anti-cancer research.

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Tubulin polymerization-IN-28 Chemical Structure

Tubulin polymerization-IN-28 Chemical Structure

CAS No. : 2481404-89-9

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Tubulin polymerization-IN-28 Related Antibodies

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Description

Tubulin polymerization-IN-28 (compound-4) is a microtubule protein polymerization inhibitor with highly selective anticancer activity. Tubulin polymerization-IN-28 can be activated by NQO1 and effectively release combretastatin A-4 to kill tumor cells. Tubulin polymerization-IN-28 can induce cell apoptosis and be used in anti-cancer research[1].

In Vitro

Tubulin polymerization-IN-28 (compound-4) (9-381 nM，48 hours)has a significant inhibitory effect on tumor cells[1].
Tubulin polymerization-IN-28 (compound-4) (10 nM，48 hours) inhibits microtubule assembly with anti-tumor activity[1].
Tubulin polymerization-IN-28 (compound-4) (10 nM，48 hours) causes G2/M phase arrest in cells[1].
Tubulin polymerization-IN-28 (compound-4) (10 nM，24 hours) leads to significant cell apoptosis[1].

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

Tubulin polymerization-IN-28 Related Antibodies

Cell Proliferation Assaysup>[1]

Cell Line: NQO1-Overexpressing A549, HepG2; Hypoxia-exposed A549 (A549/Hyp), HepG2 (HepG2/Hyp) cells; Taxol-resistant A549 cells (A549/T)
Concentration: 9-381 nM
Incubation Time: 48 hours
Result: Inhibited A549, HepG2, A549/Hyp, HepG2/Hyp, A549/T with IC50values of 10 nM, 26 nM, 72 nM, 85 nM, 56 nM, 74 nM and 88 nM respectively.

Immunofluorescencesup>[1]

Cell Line: HepG2
Concentration: 10 nM
Incubation Time: 48 hours
Result: Showed that Tubulin polymerization-IN-28 converted to CA-4, thereby inhibiting microtubule assembly, in the presence of NQO1.

Cell Cycle Analysis[1]

Cell Line: HepG2
Concentration: 0 nM，10 nM
Incubation Time: 48 hours
Result: Resulted in an increase in the percentage of G2/M phase cells from 12.71% to 33.49%.

Apoptosis Analysis[1]

Cell Line: HepG2
Concentration: 0 nM，10 nM
Incubation Time: 24 hours
Result: Showed the apoptosis rate of cells increasing from 6.54% to 23.93%.
In Vivo

Tubulin polymerization-IN-28 (compound-4) (intraperitoneal injection, every day, 17days) exhibits good anti-cancer activity in HepG2 xenograft-bearing BALB/c mice model in vivo[1].

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

Animal Model: HepG2 xenograft-bearing BALB/c mice[1]
Dosage: 20 mg/kg, 40 mg/kg
Administration: Intraperitoneal injection; every day; 17days
Result: Resulted in 47.49% reduction in tumor growth at a concentration of 20 mg/kg. Resulted in 54.87% reduction in tumor growth at a concentration of 40 mg/kg.
Molecular Weight

662.77

Formula

C37H46N2O9
CAS No.
SMILES

COC1=CC(/C=C\C2=CC(OC)=C(C=C2)OC(N(CCN(C(CC(C)(C3=C(C(C(C)=C(C3=O)C)=O)C)C)=O)C)C)=O)=CC(OC)=C1OC
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References
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Tubulin polymerization-IN-28 Related Classifications

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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.

Keywords:

Tubulin polymerization-IN-282481404-89-9Microtubule/TubulinApoptosisCombretastatin A-4NQO1-activatable prodrugAntitumorMicrotubulinInhibitorinhibitorinhibit

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