Tubulin polymerization-IN-88
Tubulin polymerization-IN-88 is a tubulin inhibitor that blocks tubulin polymerization, leading to microtubule destabilization and disruption of the mitotic spindle. Tubulin polymerization-IN-88 induces G2/M phase arrest and apoptosis in cancer cells, and inhibits cancer cell migration and self-renewal of cancer stem cells. It exhibits in vitro anti-proliferative activity against cancer cells with selectivity over normal cells. Tubulin polymerization-IN-88 also demonstrates in vivo anti-cancer activity without significant toxicity. Tubulin polymerization-IN-88 is applicable for research on glioblastoma, lung cancer, endometrial cancer, ovarian cancer, and leukemia.
For research use only. We do not sell to patients.
- Formula: C30H39N3O3S
- Molecular Weight:521.71
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
|
Bcl-xL |
Tubulin polymerization-IN-88 (compound 9b) (72 h) potently inhibits the proliferation of GBM (U87 MG, A172, U118 MG), lung cancer (A549), ovarian cancer (SKOV3), leukemia (K562, HL60), and other cancer cell lines with IC50 values ranging from 0.27 to 12.45 μM, while being non-toxic to normal 293T cells[1].
Tubulin polymerization-IN-88 (1-30 μM; 24 h) induces dose-dependent apoptosis in U118 MG cells at concentrations ≥3 μM and downregulates Bcl-XL expression[1].
Tubulin polymerization-IN-88 (0.1-1 μM; 24-72 h) potently inhibits U118 MG cell migration in concentration- and time-dependent manners via both scratch wound healing and transwell assays[1].
Tubulin polymerization-IN-88 (1-30 μM; 3 days) efficiently represses self-renewal of U118 MG cancer stem cells by reducing neurosphere formation and downregulating CD133 and SOX2 expression[1].
Tubulin polymerization-IN-88 (1-30 μM; 24 h) induces G2/M phase arrest in U118 MG cells via downregulation of Cyclin B1 and CDK1[1].
Tubulin polymerization-IN-88 (1-30 μM; 24 h) disrupts tubulin polymerization and spindle microtubule assembly in U118 MG cells, leading to reduced α/β-tubulin expression[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:U87 MG, A172, U118 MG, A549, ISK, SKOV3, U251, K562, HL60, 293T
-
Concentration:varied for IC₅₀ determination
-
Incubation Time:72 h
-
Result:Inhibited proliferation of U87 MG cells with an IC50 of 0.27 μM; inhibited proliferation of A172 cells with an IC50 of 1.22 μM; inhibited proliferation of U118 MG cells with an IC50 of 0.88 μM; inhibited proliferation of A549 cells with an IC50 of 0.33 μM; inhibited proliferation of ISK cells with an IC50 of 12.45 μM; inhibited proliferation of SKOV3 cells with an IC50 of 0.47 μM; inhibited proliferation of U251 cells with an IC50 of 1.29 μM; inhibited proliferation of K562 cells with an IC50 of 0.73 μM; inhibited proliferation of HL60 cells with an IC50 of 2.02 μM; showed negligible toxicity to 293T cells with an IC50 >100 μM.
-
Cell Line:U118 MG
-
Concentration:1, 3, 10, 30 μM
-
Incubation Time:24 h
-
Result:Induced dose-dependent increase in total apoptotic cells, with statistical significance at and above 3 μM; downregulated anti-apoptotic protein Bcl-XL in a concentration-dependent manner.
-
Cell Line:U118 MG
-
Concentration:0.1, 0.3, 1 μM
-
Incubation Time:24, 48, 72 h (scratch assay); 24 h (transwell assay)
-
Result:Inhibited scratch wound closure in a concentration- and time-dependent manner (significant inhibition at 72 h); dose-dependently reduced transwell migration.
-
Cell Line:U118 MG
-
Concentration:1, 3, 10, 30 μM
-
Incubation Time:24 h
-
Result:Induced G2/M phase arrest at low concentrations (1-10 μM); dose-dependently reduced expression of cell cycle regulators Cyclin B1 and CDK1.
-
Cell Line:U118 MG
-
Concentration:1, 3, 10, 30 μM
-
Incubation Time:24 h
-
Result:Significantly reduced α/β-tubulin protein
expression in U118 MG cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:BALB/c nude (male, 6-7 weeks old, 16-19 g, U118 MG xenograft model)[1]
-
Dosage:2.5, 8, 20 mg/kg
-
Administration:i.p.; daily; 28 days
-
Result:Suppressed tumor growth dose-dependently; induced 49.7% tumor weight growth inhibition (TGI) at 8 mg/kg, and 49.8% TGI at 20 mg/kg (both statistically significant vs control); caused no significant body weight loss or overt toxicity.
Chemical Information
-
Molecular Weight 521.71
-
Formula C30H39N3O3S
-
SMILES
O=C(NC(S1)=NC2=C1CN(CC3=C[C@]4(O)[C@H](C(C)C)C[C@]5(O4)[C@@H](C)CCC35)CC2)C6=CC=CC(C)=C6C
-
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
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Tubulin polymerization-IN-88 Related Classifications
HY-181074 Related Classifications
Powered by Bioz