2. Cell Cycle/DNA Damage Cytoskeleton Apoptosis
  3. Microtubule/Tubulin Apoptosis Bcl-2 Family
  4. 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.

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Tubulin polymerization-IN-88

Tubulin polymerization-IN-88 Chemical Structure

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Tubulin polymerization-IN-88 Related Antibodies

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Description

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[1].

IC50 & Target[1]

Bcl-xL

 

In Vitro

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.

Tubulin polymerization-IN-88 Related Antibodies

Cell Viability Assay[1]

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.

Apoptosis Analysis[1]

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 Migration Assay [1]

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 Cycle Analysis[1]

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.

Western Blot Analysis[1]

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.
Parmacokinetics
Species Dose Route Cmax Tmax AUC0-inf T1/2 MRT0-inf F
Rat[1] 5 mg/kg i.v. 3241 ng/mL / 651 ng·h/mL 1.03 h 0.264 h /
Rat[1] 10 mg/kg i.p. 271 ng/mL 0.25 h 407 ng·h/mL 1.20 h 1.46 h 40.8 %
In Vivo

Tubulin polymerization-IN-88 (compound 9b) (2.5-20 mg/kg; i.p.; daily; 28 days) exhibits potent dose-dependent in vivo anti-glioblastoma activity with 49.7-49.8% tumor weight growth inhibition (TGI) and an acceptable safety profile[1].

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.
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
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Tubulin polymerization-IN-88 Related Classifications

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Help & FAQs
  • 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-88Microtubule/TubulinApoptosisBcl-2 Familyendometrial cancercancer stem cellsG2/M-phase arrestlung cancermitotic spindleglioblastomaovarian cancermicrotubuletubulinleukemiaInhibitorinhibitorinhibit

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