2. Cell Cycle/DNA Damage Cytoskeleton Apoptosis
  3. Microtubule/Tubulin Apoptosis
  4. WX-132-18B

WX-132-18B is a tubulin inhibitor with an IC50 of 0.45-0.99 nM. WX-132-18B selectively binds to the colchicine-binding site on tubulin, reduces microtubule content via depolymerization, and inhibits tubulin polymerization. WX-132-18B induces tumor cell cycle arrest, apoptosis and changes in nuclear membrane permeability, and decreases mitochondrial membrane potential. WX-132-18B exhibits antiproliferative activity against endothelial cells and human tumor cells, and inhibits the proliferation and growth of xenograft tumors in mice. WX-132-18B can be used in research related to sarcoma, non-small cell lung cancer, gastric cancer and breast cancer.

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

WX-132-18B

WX-132-18B Chemical Structure

CAS No. : 1415262-07-5

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

WX-132-18B Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

WX-132-18B is a tubulin inhibitor with an IC50 of 0.45-0.99 nM. WX-132-18B selectively binds to the colchicine-binding site on tubulin, reduces microtubule content via depolymerization, and inhibits tubulin polymerization. WX-132-18B induces tumor cell cycle arrest, apoptosis and changes in nuclear membrane permeability, and decreases mitochondrial membrane potential. WX-132-18B exhibits antiproliferative activity against endothelial cells and human tumor cells, and inhibits the proliferation and growth of xenograft tumors in mice. WX-132-18B can be used in research related to sarcoma, non-small cell lung cancer, gastric cancer and breast cancer[1][2].

IC50 & Target[1]

β-Tubulin

0.47 μM (IC50)

In Vitro

WX-132-18B (72 h) potently inhibits the proliferation of HepG2, HeLa, A549, H460, BGC-823, MX-1, taxol-resistant MX-1/T, and HUVEC cells with IC50 values ranging from 0.45 to 0.99 nM[1].
WX-132-18B (1-10 nM; 24 h) reduces tubulin content and altering tubulin morphology with EC50 values ranging from 2.99 to 9.43 nM[1].
WX-132-18B (0.1-10 μM; 45 min pre-incubation with tubulin, 45 min incubation with colchicine) competitively binds to the colchicine-binding site on tubulin with an IC50 of 0.47 μM[1].
WX-132-18B (1-10 nM; 24-48 h) potently arrests A549 cells at the G2/M phase of the cell cycle within 24 h, induces concentration-dependent apoptosis in A549 cells after 48 h, and triggers concentration-dependent cytotoxicity in HepG2 cells at 24 h by increasing nuclear membrane permeability while reducing manganese superoxide dismutase levels and mitochondrial membrane potential[1].
WX-132-18B (0.03-3 μM; per manufacturer instructions) exhibits high target selectivity, with no significant effect on 21 screened tumor-related signaling pathways and only weak, non-specific DNA damage (Rad51 foci induction) at high concentrations[1].
WX-132-18B (compound 2) displays broad-spectrum and ultra-potent antiproliferative activity with low-to-subnanomolar GI50 values across most NCI-60 human tumor cell lines, although its potency is decreased in HOP-92, MALME-3M, SK-MEL-28, UACC-257, OVCAR-5, and TK-10 cells. It also strongly inhibits the growth of A549, KB, and KB-VIN cells with GI50 values of 2.20-3.20 nM[2].
WX-132-18B (15 min preincubation; 20 min incubation with GTP) inhibits purified tubulin polymerization with an IC50 of 0.77 μM[2].

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

WX-132-18B Related Antibodies

Cell Cycle Analysis[1]

Cell Line: A549
Concentration: 1, 3, 10 nM
Incubation Time: 24 h
Result: Induced cell cycle arrest at the G2/M phase in a concentration-dependent manner.
Resulted in 74.77% of cells in the G2/M phase when treated with 3 nM WX-132-18B, compared to 8.68% in the control group.

Apoptosis Analysis[1]

Cell Line: A549
Concentration: 1, 3, 10 nM
Incubation Time: 48 h
Result: Induced A549 cell apoptosis in a concentration-dependent manner.
Produced an apoptotic effect equivalent to that of control microtubule inhibitors (300 nM Colchicine (HY-16569), 300 nM Vincristine (HY-N0488A), 100 nM taxol) when treated with 3 nM WX-132-18B, with significant increases in both early and late apoptotic cell populations.

Cell Cytotoxicity Assay[1]

Cell Line: HepG2
Concentration: 3 nM
Incubation Time: 24 h
Result: Induced concentration-dependent cytotoxic effects including reduced cell count, reduced nuclear size, increased NMP, reduced MnSOD levels, and reduced MMP.
Produced a cytotoxic profile similar to 300 nM Colchicine, 300 nM Vincristine, and 100 nM taxol at 3 nM, with stronger effects on MnSOD and MMP reduction, and weaker effects on NMP increase, compared to taxol or vincristine.
In Vivo

WX-132-18B (0.25-1.0 mg/kg; i.p.; twice a week; 3 weeks) dose-dependently inhibits sarcoma S180 xenograft growth in KM mice[1].
WX-132-18B (0.25-1.0 mg/kg; i.p.; twice a week; 3 weeks) dose-dependently inhibits BGC-823 human gastric cancer xenograft growth in nude mice via inducing apoptosis, inhibiting cell proliferation, and suppressing angiogenesis[1].
WX-132-18B (0.25-1.0 mg/kg; i.p.; once every 5 days; 3 weeks) dose-dependently inhibits H460 human non-small cell lung cancer xenograft growth in nude mice[1].
WX-132-18B (compound 2) (0.25-1.0 mg/kg; i.v.; every 5 days; 3 weeks) exhibits dose-dependent in vivo antitumor activity against NCI-H460 xenografts[2].

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

Animal Model: Kunming (KM) mice (6- to 8-week-old; subcutaneous S180 sarcoma model)[1]
Dosage: 0.25 mg/kg; 0.5 mg/kg; 1.0 mg/kg
Administration: i.p.; twice a week; 3 weeks
Result: Induced 70.06% inhibition of tumor volume at 1.0 mg/kg.
Induced 72.62% inhibition of tumor weight at 1.0 mg/kg.
Inhibited tumor growth in a dose-dependent manner.
Animal Model: Nude mice (Nu/Nu) (8-week-old; subcutaneous H460 non-small cell lung cancer model)[1]
Dosage: 0.25 mg/kg; 0.5 mg/kg; 1.0 mg/kg
Administration: i.p.; once every 5 days; 3 weeks
Result: Induced 68.70% inhibition of tumor volume at 1.0 mg/kg.
Induced 61.90% inhibition of tumor weight at 1.0 mg/kg.
Exhibited anti-tumor effect comparable to that of 15 mg/kg taxol at 1.0 mg/kg.
Animal Model: Nude mice (Nu/Nu) (8-week-old; subcutaneous BGC-823 gastric cancer model)[1]
Dosage: 0.25 mg/kg; 0.5 mg/kg; 1.0 mg/kg
Administration: i.p.; twice a week; 3 weeks
Result: Induced 76.06% inhibition of tumor volume at 1.0 mg/kg.
Induced 77.32% inhibition of tumor weight at 1.0 mg/kg.
Caused shrunken, structurally incomplete nuclei in treated tumor tissues versus enlarged, deeply stained nuclei in controls.
Increased caspase 3 expression, reduced Ki67 expression, and reduced CD31 expression in a dose-dependent manner.
Animal Model: Balb/c-nu nude mice (female, 6 weeks old)[2]
Dosage: 0.25 mg/kg; 0.5 mg/kg; 1.0 mg/kg
Administration: i.v.; every 5 days; 3 weeks
Result: Reduced mean tumor weight and increased tumor growth inhibition in a dose‑dependent manner: 17.8% (2.23 g) at 0.25 mg/kg, 36.8% (1.72 g) at 0.5 mg/kg, and 61.9% (1.03 g) at 1.0 mg/kg.
Reduced vessel size and number via CD31 staining.
Increased cleaved caspase-3 staining, indicating apoptosis.
Decreased Ki67 staining, indicating reduced tumor cell proliferation.
Molecular Weight

320.35

Formula

C18H16N4O2
CAS No.
SMILES

O=C1NC2=CC(OC)=CC=C2N(C=3N=C(N=C4C=CC=CC43)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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

WX-132-18B Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
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:

WX-132-18B1415262-07-5Microtubule/TubulinApoptosisHepG2endothelial cellstaxol-resistant breast cancer cellstumor cell apoptosiscolchicine-binding sitehuman tumor cellsmicrotubuletubulinG2/M phaseHeLaInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
WX-132-18B
Cat. No.:
HY-138008
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.