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Cat. No.: HY-189398

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Tubulin polymerization-IN-94

Tubulin polymerization-IN-94 is a tubulin polymerization inhibitor. Tubulin polymerization-IN-94 inhibits tubulin polymerization, forms a hydrogen bond with β-Asn349, and exhibits π-stacking with β-Lys352. Tubulin polymerization-IN-94 shows potent antiproliferative activity against multiple cancer cell lines. Tubulin polymerization-IN-94 induces G₂/M cell cycle arrest, apoptosis, and disruption of the microtubule network. Tubulin polymerization-IN-94 can be used in research related to cervical cancer, gastric cancer, and breast cancer.

For research use only. We do not sell to patients.

Formula: C₂₂H₁₉N₅O₃
Molecular Weight:401.42

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Tubulin polymerization-IN-94 Chemical Structure

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- Cellular Effect
- In Vitro
Chemical Information
Purity & Documentation
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Biological Activity

Description

Cellular Effect

Cell Line	Type	Value	Description	References
HeLa	IC50	0.13 μM	Antiproliferative activity against human HeLa cervical carcinoma cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay. Antiproliferative activity against human HeLa cervical carcinoma cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.	42621831
SGC-7901	IC50	0.15 μM	Antiproliferative activity against human SGC-7901 gastric carcinoma cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay. Antiproliferative activity against human SGC-7901 gastric carcinoma cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.	42621831
MCF7	IC50	0.18 μM	Antiproliferative activity against human MCF-7 breast carcinoma cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay. Antiproliferative activity against human MCF-7 breast carcinoma cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.	42621831
HUVEC	IC50	4.5 μM	Cytotoxicity against normal human umbilical vein endothelial cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay. Cytotoxicity against normal human umbilical vein endothelial cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.	42621831

In Vitro

Anti-cancerCell Cycle RegulationApoptosisOthers

Anti-cancer

Tubulin polymerization-IN-94 (Compound 10t) (0-100 μM; 72 h) exhibits potent antiproliferative activity against HeLa, SGC-7901, and MCF-7 cancer cell lines with IC₅₀ values of 0.13, 0.15, and 0.18 μM, respectively, and shows good cancer cell selectivity with low cytotoxicity against normal HUVECs^[1].

Anti-cancer

Cell Cycle Regulation

Tubulin polymerization-IN-94 (130 nM; 24 h) effectively disrupts microtubule stability and interferes with normal mitotic progression in HeLa cells, inducing microtubule depolymerization, nuclear condensation, and multinucleation^[1].

Cell Cycle Regulation

Anti-cancer

Tubulin polymerization-IN-94 (65-260 nM; 24 h) effectively disrupts normal mitotic progression in HeLa cells by inducing dose-dependent G₂/M phase arrest^[1].

Apoptosis

Anti-cancer

Tubulin polymerization-IN-94 (65-260 nM; 48 h) efficiently induces apoptosis in HeLa cervical cancer cells in a dose-responsive manner^[1].

Others

Tubulin polymerization-IN-94 (3 μM; 0-60 min) acts as a potent microtubule destabilizer by inhibiting tubulin polymerization^[1].
Tubulin polymerization-IN-94 binds to the colchicine site of tubulin with a docking score of −10.467 and forms a unique hydrogen bond with β-Asn349, which is not observed for CA-4 or compound 7^[1].
Tubulin polymerization-IN-94 (100 ns) forms a dynamically stable complex with tubulin at the colchicine binding site, with low ligand RMSD and stable protein conformation^[1].
Tubulin polymerization-IN-94 complies with Lipinski's rule and exhibits favorable drug-like properties, suggesting potential oral bioavailability^[1].

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

Immunofluorescence^[1]

Cell Line:

HeLa
Concentration:

130 nM
Incubation Time:

24 h
Result:

Caused pronounced disruption of the microtubule network.
The filamentous structures broke down and collapsed, giving rise to dense, perinuclear aggregates surrounding the nucleus.
Marked nuclear pyknosis, indicative of chromatin condensation, along with the emergence of multinucleated cells, was clearly observed.

Cell Cycle Analysis^[1]

Cell Line:

HeLa
Concentration:

65, 130 and 260 nM
Incubation Time:

24 h
Result:

Induced a dose-dependent and marked accumulation of cells within the G₂/M phase.
The percentage of cells arrested at G₂/M rose from 4.05% in the vehicle control group to as high as 80.69% at the highest tested concentration.

Apoptosis Analysis^[1]

Cell Line:

HeLa
Concentration:

65, 130 and 260 nM
Incubation Time:

48 h
Result:

Induced a marked, concentration-dependent increase in apoptosis.
At 65 nM, total apoptosis rate was 4.9% (0.5% early, 4.4% late), with 2.2% necrosis and 92.9% viable cells.
At 130 nM, total apoptosis increased to 8.6% (2.3% early, 6.3% late), with 5.2% necrosis and 86.2% viable cells.
At 260 nM, total apoptosis reached 18.5% (5.5% early, 13.0% late), with 4.4% necrosis and 77.1% viable cells.

Related Protocols :

Chemical Information

Molecular Weight 401.42
Formula C₂₂H₁₉N₅O₃
SMILES

COC(C(OC)=C1)=C(OC)C=C1N2N=CC3=NC=C(C4=CC=CC5=C4C=CN5)N=C32
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

Handling Instructions (2659 KB)

References

[1]. Guo Z, et al. Conformationally constrained 6‑aryl‑1‑(3,4,5‑trimethoxyphenyl)-1-pyrazolo[3,4‑b]pyrazines as novel microtubule destabilizers: design, synthesis, and antitumor evaluation. Journal of enzyme inhibition and medicinal chemistry. 2026 Dec;41(1):2717975.

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biological Activity
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Tubulin polymerization-IN-94

Biological Activity

Description

Cellular Effect

In Vitro

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

Tubulin polymerization-IN-94 Related Classifications

HY-189398 Related Classifications

Bioz

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