Tubulin polymerization-IN-93
Tubulin polymerization-IN-93 is a β-tubulin polymerization inhibitor. Tubulin polymerization-IN-93 disrupts the microtubule network structure. Tubulin polymerization-IN-93 activates the spindle assembly checkpoint and promotes Mitotic catastrophe. Tubulin polymerization-IN-93 activates the mitochondrial Apoptotic pathway. Tubulin polymerization-IN-93 exhibits anticancer activity against acute myeloid leukemia.
For research use only. We do not sell to patients.
- CAS No.: 3022872-60-9
- Formula: C22H23NO6
- Molecular Weight:397.42
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Tubulin polymerization-IN-93 (Compound III-3) (0-150 nM; 24-72 h) potently and selectively inhibits the viability of AML cell lines MV-4-11, HL-60 and THP-1 with IC50 values ranging from 74.25 to 92.20 nM, while exhibiting low toxicity toward normal cells[1].
Tubulin polymerization-IN-93 (10 μM; 12 h) directly binds to β-tubulin in AML MV-4-11 and HL-60 cells, protecting it from protease-mediated degradation[1].
Tubulin polymerization-IN-93 (10 μM; 3 h) directly binds to β-tubulin in AML MV-4-11 and HL-60 cells and increases its thermal stability[1].
Tubulin polymerization-IN-93 (1-10 μM; 2 h) competes with EBI for binding to the colchicine-binding site on β-tubulin in AML MV-4-11 and HL-60 cells[1].
Tubulin polymerization-IN-93 (150 nM; 12-24 h) induces abnormal spindle formation and multinucleated cells, thereby triggering mitotic catastrophe in AML MV-4-11 and HL-60 cells[1].
Tubulin polymerization-IN-93 (150 nM; 24 h) induces DNA damage in acute myeloid leukemia MV-4-11 and HL-60 cells[1].
Tubulin polymerization-IN-93 (75-150 nM; 12 h) induces G2/M phase arrest in AML MV-4-11 and HL-60 cells[1].
Tubulin polymerization-IN-93 (75-150 nM; 12 h) activates the spindle assembly checkpoint in AML MV-4-11 and HL-60 cells, upregulates the expression of MAD1, MAD2, BUBR1, PTTG1 and Cyclin B1, and downregulates the expression of p-CDK1Tyr15[1].
Tubulin polymerization-IN-93 (75-150 nM; 24 h) induces apoptosis in AML MV-4-11 and HL-60 cells in a concentration-dependent manner, with an apoptosis rate exceeding 80% after treatment at 150 nM for 24 h[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human AML MV-4-11, HL-60, THP-1 cells; human normal HUVEC, LO2, PBMC cells
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Concentration:0-150 nM
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Incubation Time:24 h, 48 h, 72 h
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Result:Exhibited potent, time- and concentration-dependent antiproliferative activity against AML cells, with IC50 values of 74.25 nM (MV-4-11), 87.99 nM (HL-60), and 92.20 nM (THP-1).
Showed low toxicity to normal human cells (HUVEC, LO2, PBMC).
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Cell Line:human AML MV-4-11 and HL-60 cells
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Concentration:75-150 nM
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Incubation Time:12 h (after 12 h starvation)
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Result:Significantly increased the percentage of cells in G2/M phase compared to synchronized control cells.
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Cell Line:human AML MV-4-11 and HL-60 cells
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Concentration:75-150 nM
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Incubation Time:12 h
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Result:Significantly upregulated the expression of pHH3, an M-phase marker.\nDose-dependently upregulated the expression of MAD1, MAD2, BUBR1, PTTG1, and Cyclin B1.
Downregulated p-CDK1(Tyr15) levels.
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Cell Line:human AML MV-4-11 and HL-60 cells
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Concentration:75-150 nM
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Incubation Time:24 h
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Result:Concentration-dependently increased apoptosis rates.
Achieved apoptosis rates of 80.83% (MV-4-11) and 83.00% (HL-60) after treatment with 150 nM for 24 h.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c-nu nude (female, 5-6 weeks old, subcutaneous xenograft model)[1]
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Dosage:5 mg/kg; 20 mg/kg
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Administration:i.p.; every 2 days; 16 days
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Result:Produced a tumor inhibition rate of 41.42% at 5 mg/kg.
Produced a tumor inhibition rate of 71.40% at 20 mg/kg.
Did not induce significant mouse weight loss or major organ damage (liver, heart, spleen, lungs, kidneys) at both doses.
Significantly increased tumor tissue necrosis area in both treatment groups.
Significantly downregulated tumor proliferation markers Ki67 and PCNA in both treatment groups.
Significantly upregulated spindle assembly checkpoint-related proteins pHH3, MAD2, and BUBR1 in both treatment groups.
Significantly downregulated anti-apoptotic protein MCL-1 in both treatment groups.
Chemical Information
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CAS No. 3022872-60-9
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Molecular Weight 397.42
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Formula C22H23NO6
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SMILES
COC1=CC(N(C(C2=CC=CO2)=O)CC3=CC=C(OC)C=C3)=CC(OC)=C1OC
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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)
Tubulin polymerization-IN-93 Related Classifications
HY-184760 Related Classifications
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- Tubulin polymerization-IN-93
- 3022872-60-9
- Microtubule/Tubulin
- Mitosis
- Apoptosis
- Mitochondrial Metabolism
- microtubule network structure
- colchicine-binding site
- HL-60 cells
- spindle assembly checkpoint
- M-phase arrest
- mitotic catastrophe
- leukemia cells
- acute myelocytic leukemia
- β-tubulin
- MV-4-11 cells
- Inhibitor
- inhibitor
- inhibit