2. Cell Cycle/DNA Damage Cytoskeleton Metabolic Enzyme/Protease Apoptosis
  3. Microtubule/Tubulin Phosphatase Apoptosis
  4. Tubulin-IN-62

Tubulin-IN-62 is a tubulin inhibitor targeting the colchicine-binding site. Tubulin-IN-62 exhibits IC50 values of 17.2 nM and 19.3 nM against SKOV3 and HCC827 cells, respectively. Tubulin-IN-62 inhibits microtubule polymerization, arrests the cell cycle at the G2/M phase, and induces apoptosis. Tubulin-IN-62 demonstrates significant antitumor efficacy in vivo with good tolerability. Tubulin-IN-62 can be used in ovarian cancer and non-small cell lung cancer (NSCLC) research.

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Tubulin-IN-62

Tubulin-IN-62 Chemical Structure

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Tubulin-IN-62 Related Antibodies

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Description

Tubulin-IN-62 is a tubulin inhibitor targeting the colchicine-binding site. Tubulin-IN-62 exhibits IC50 values of 17.2 nM and 19.3 nM against SKOV3 and HCC827 cells, respectively. Tubulin-IN-62 inhibits microtubule polymerization, arrests the cell cycle at the G2/M phase, and induces apoptosis. Tubulin-IN-62 demonstrates significant antitumor efficacy in vivo with good tolerability. Tubulin-IN-62 can be used in ovarian cancer and non-small cell lung cancer (NSCLC) research[1].

In Vitro

Tubulin-IN-62 (compound (S)-Q31) (10-80 nM, 10 days) inhibits colony-formation ability of SKOV3 and HCC827 cells[1].
Tubulin-IN-62 (10-80 nM, 24 h) suppresses the migration of SKOV3 and HCC827 cells[1].
Tubulin-IN-62 (10-80 nM, 48 h) exerts antiproliferative effect and induces apoptosis in SKOV3 and HCC827 cells[1].
Tubulin-IN-62 (5-40 nM, 48 h) induces apoptosis in SKOV3 and HCC827 cells[1].
Tubulin-IN-62 (10-80 nM, 24 h) arrests SKOV3 and HCC827 cells at the G2/M phase[1].
Tubulin-IN-62 (10-80 nM, 48 h) induces G2/M phase cell cycle arrest by downregulating the expression of Cdc-25c, cyclin B1, and Cdc-2 in SKOV3 and HCC827 cells [1].
Tubulin-IN-62 (2.5-20 μM, 80 min) exhibits inhibitory activity on tubulin polymerization in SKOV3 and HCC827 cells[1].
Tubulin-IN-62 (40 nM, 24 h) inhibits microtubule polymerization and disrupts microtubule networks in SKOV3 and HCC827 cells[1].

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

Tubulin-IN-62 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: SKOV3 and HCC827 cell lines
Concentration: 10, 20, 40, 80 nM
Incubation Time: 10 Days
Result: Reduced both the colony number and area in both SKOV3 and HCC827 cells in a dose-dependent manner, with complete inhibition of clonogenic potential observed at 40 nM.

Cell Migration Assay [1]

Cell Line: SKOV3 and HCC827 cell lines
Concentration: 0, 10, 20, 40, and 80 nM
Incubation Time: 24 h
Result: Inhibited the migration of SKOV3 cells in a dose-dependent manner after 24 h.
Reduced the number of migrated cells from 4110 (untreated control) to 2433, representing 59.0 % of the control level in SKOV3 cells.
Reduced the number of migrated cells from 332 (untreated control) to 60 at 80 nM in HCC827 cells.
Inhibited the wound closure rate from 52.8% to 7.5 % in SKOV3 cells.
Decreased the closure rate from 70.4 % to 13.1 % in HCC827 cells.
Induced significant cytotoxicity alongside the observed inhibition at this highest concentration.

Apoptosis Analysis[1]

Cell Line: SKOV3 and HCC827 cell lines
Concentration: 10, 20, 40, 80 nM
Incubation Time: 48 h
Result: Resulted in dose-dependent increases in the total apoptosis rates in SKOV3 cells, reaching 11.29 %, 24.80 %, 32.65 %, and 35.11 % at 10, 20, 40, and 80 nM, respectively.
Increased the apoptosis rates from 2.80 % (control) to 3.23 %, 6.10 %, 6.56 %, and 16.01 % at t10, 20, 40, and 80 nM, respectively in HCC827 cells.

Western Blot Analysis[1]

Cell Line: SKOV3 and HCC827 cell lines
Concentration: 5, 10, 20, 40nM
Incubation Time: 48 h
Result: Reduced the expression of the anti-apoptotic protein Bcl-2 and dose dependently upregulated the levels of pro-apoptotic proteins Cleaved PARP, Cleaved Caspase-9, Cleaved Caspase-3, and Bax in both SKOV3 and HCC827 cells.

Cell Cycle Analysis[1]

Cell Line: SKOV3 and HCC827 cell lines
Concentration: 10, 20, 40, 80 nM
Incubation Time: 24 h
Result: Induced dose-dependent G2/M phase arrest in SKOV3 cells, with the proportion of arrested cells rising to 25.96%, 42.01%, 76.32%, and 72.54% at 10, 20, 40, and 80 nM, respectively.
Induced G2/M phase arrest in HCC827 cells,with 30.82 %, 54.01 %, 87.16 %, and 88.24 % at 10, 20, 40, and 80 nM, respectively

Western Blot Analysis[1]

Cell Line: SKOV3 and HCC827 cell lines
Concentration: 10, 20, 40, 80 nM
Incubation Time: 48 h
Result: Reduced the expression levels of cyclin B1, Cdc-2, and Cdc-25c.
In Vivo

Tubulin-IN-62 (compound (S)-Q31) (2,4 mg/kg, i.v., every other day (q2d) for a total of 12 doses) exhibited antitumor efficacy in SKOV3 cell-induced xenograft models in female Balb/c mice by inhibiting proliferation and promoting apoptosis and induced no significant pathological alterations in major organs, indicating a favorable safety profile[1].

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

Animal Model: SKOV3 cells (5 × 106 SKOV3 cells, s.c.)-induced female Balb/c mice[1]
Dosage: 2 mg/kg or 4 mg/kg
Administration: i.v., every other day (q2d) for a total of 12 doses
Result: Demonstrated significant tumor growth inhibition (TGI), with reductions of 63.79 %, 74.12 %, and 62.94 %, respectively.
Remained body weights stable across all group.
Reduced the expression of the proliferation marker Ki-67 to a greater extent than paclitaxel, particularly at the 4 mg/ kg dose.
Decreased the expression of the anti-apoptotic protein Bcl-2 and increased the expression of the apoptosis marker cleaved PARP in a dose-dependent manner.
Molecular Weight

393.44

Formula

C21H23N5O3
SMILES

CC1=CC(C(N2)=C[C@@H](C3=CC(OC)=C(OC)C(OC)=C3)N4C2=NN=N4)=CC(C)=C1
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-IN-62 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-IN-62Microtubule/TubulinPhosphataseApoptosisantitumor agentsmultidrug resistanceOvarian CancerNon-Small Cell Lung Cancermicrotubule polymerizationinduces apoptosisInhibitorinhibitorinhibit

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