1. Metabolic Enzyme/Protease Apoptosis
  2. Glutaminase Apoptosis
  3. GLS1 Inhibitor-4

GLS1 Inhibitor-4 (compound 41e) is a potent GLS1 inhibitor with an IC50 of 11.86 nM. GLS1 Inhibitor-4 shows antiproliferative activity, good metabolic stability, robust GLS1 binding affinity. GLS1 Inhibitor-4 blocks the glutamine metabolism and induce the production of ROS. GLS1 Inhibitor-4 induces apoptosis and shows antitumor activity.

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

GLS1 Inhibitor-4 Chemical Structure

GLS1 Inhibitor-4 Chemical Structure

CAS No. : 2768599-97-7

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  
Synthetic products have potential research and development risk.

* Please select Quantity before adding items.

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

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

GLS1 Inhibitor-4 (compound 41e) is a potent GLS1 inhibitor with an IC50 of 11.86 nM. GLS1 Inhibitor-4 shows antiproliferative activity, good metabolic stability, robust GLS1 binding affinity. GLS1 Inhibitor-4 blocks the glutamine metabolism and induce the production of ROS. GLS1 Inhibitor-4 induces apoptosis and shows antitumor activity[1].

IC50 & Target

IC50: 11.86 nM (GLS1)[1]

In Vitro

GLS1 Inhibitor-4 (compound 41e) shows antiproliferative activity with IC50s of 0.051, 0.37, 0.32, 1.34 µM for HCT116 and MDA-MB-436, CT26, H22 cells, respectively[1].
GLS1 Inhibitor-4 shows good plasma and liver microsomal stability with 96% stability in Human plasma[1].
GLS1 Inhibitor-4 shows robust binding affinity with GLS1 protein, the dissociation constants (Kd) of 52 nM[1].
GLS1 Inhibitor-4 (0.1, 0.5, 1 µM) inhibits the colony formation of HCT116 cells in a dose-dependent manner[1].
GLS1 Inhibitor-4 (100, 300 nM, 12 h) reduces the concentration of a number of key metabolites downstream of glutamate within 12 h[1].
GLS1 Inhibitor-4 (30, 50, 200 nM; 6 h) increases the ROS levels in a dose-dependent manner in HCT116 cells[1].
GLS1 Inhibitor-4 (1 mmol/L; 12 h) significantly decreases the ATP production basal and maximal OCRs (oxygen consumption rates) after 12 h, suppresses the aerobic glycolysis in HCT116 cancer cells[1].
GLS1 Inhibitor-4 (30, 50, 200 nM; 24 h) induces apoptosis in a dose-dependent manner[1].

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

Apoptosis Analysis[1]

Cell Line: HCT116 cells
Concentration: 30, 50, 200 nM
Incubation Time: 24 h
Result: Induced approximately 28% and 95% more apoptotic cells at concentrations of 50 and 200 nM, respectively. And upregulated the expression of apoptotic protein cleaved PARP in a dose-dependent manner.
In Vivo

GLS1 Inhibitor-4 (50, 100 mg/kg; i.p.; twice a day for 21 consecutive days) shows antitumor activity in a dose-dependent manne[1].

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

Animal Model: Six-week-old BALB/c SPF nude mice (HCT116 tumor nude mouse xenograft model)[1]
Dosage: 50, 100 mg/kg
Administration: I.p.; twice a day for 21 consecutive days
Result: Inhibited the tumor growth at a dose-dependent manne with the tumor growth inhibition (TGI) values of 35.5% at 50 mg/kg and 47.5% at 100 mg/kg, respectively.
Molecular Weight

668.72

Formula

C29H27F3N10O2S2

CAS No.
SMILES

O=C(NC1=NN=C(S1)N2CCC(CC2)NC3=NN=C(S3)NC(CC4=CC=CC=C4)=O)C5=NC=CN5CC(C=C6)=CC=C6C(F)(F)F

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
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.

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-4
Cat. No.:
HY-146617
Quantity:
MCE Japan Authorized Agent: