1. Metabolic Enzyme/Protease
    Apoptosis
  2. Glutaminase
    Apoptosis
  3. GLS1 Inhibitor-5

GLS1 Inhibitor-5 

Cat. No.: HY-151163
Handling Instructions

GLS1 Inhibitor-5 (compound 24y) is an orally active selective glutaminase 1 (GLS1) inhibitor with an IC50 value of 68 nM. GLS1 Inhibitor-5 induces apoptosis and has anti-tumor activity.

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

GLS1 Inhibitor-5 Chemical Structure

GLS1 Inhibitor-5 Chemical Structure

Size Stock
100 mg   Get quote  
250 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

GLS1 Inhibitor-5 (compound 24y) is an orally active selective glutaminase 1 (GLS1) inhibitor with an IC50 value of 68 nM. GLS1 Inhibitor-5 induces apoptosis and has anti-tumor activity[1].

In Vitro

GLS1 Inhibitor-5 (compound 24y) (0-10 μM, 48 h) can induce cell cycle arrest in the G1 phase in a dose-dependent manner, induce apoptosis and inhibit cancer cell proliferation[1].

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

Cell Proliferation Assay[1]

Cell Line: A549 and HCT116 cells
Concentration: 0-8 μM
Incubation Time:
Result: Inhibited cell proliferation with the IC50 values of 0.57 μM for A549 and 0.42 μM for HCT116, respectively.
Significantly inhibited cell clone formation.

Cell Cycle Analysis[1]

Cell Line: A549 cells
Concentration: 50-800 nM
Incubation Time: 48 hours
Result: Showed an increase in the proportion of G1 phase cells and a decrease in the proportion of S phase cells.

Apoptosis Analysis[1]

Cell Line: A549 cells
Concentration: 1-10 μM
Incubation Time: 48 hours
Result: Induced 84% of cell apoptosis at a concentration of 10 μM.
In Vivo

GLS1 Inhibitor-5 (compound 24y) (p.o., 100 mg/kg, once daily, 28 days) significantly reduces tumor growth and results in 40.9% inhibition of tumor growth at the end of the experiment in mice with A549 xenograft tumor[1].

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

Animal Model: Rats[1]
Dosage: 3 mg/kg
Administration: i.v. or p.o.
Result: The pharmacokinetic parameters of GLS1 Inhibitor-5 (compound 24y)
Parameters IV PO
t1/2 (h) 9.9 19.8
CL(L/h/kg) 6.1 33.4
Cmax(ng/mL) 699.1 41.3
AUC(0-t)(ng·h/mL) 2092.3 251.6
F(%) 12.4 12.4
Molecular Weight

660.91

Formula

C37H52N6O3S

SMILES

O=C(NCC1CCN(CCCCCC)CC1)C2=CC=CC(COCCC3CCN(C4=NN=C(NC(CC5=CC=CC=C5)=O)S4)CC3)=C2

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.
  • 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

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
GLS1 Inhibitor-5
Cat. No.:
HY-151163
Quantity:
MCE Japan Authorized Agent: