2. Metabolic Enzyme/Protease Apoptosis
  3. Glutaminase Apoptosis
  4. 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.

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GLS1 Inhibitor-4 Chemical Structure

GLS1 Inhibitor-4 Chemical Structure

CAS No. : 2768599-97-7

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GLS1 Inhibitor-4 Related Antibodies

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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.

GLS1 Inhibitor-4 Related Antibodies

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
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
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References
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GLS1 Inhibitor-4 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:

GLS1 Inhibitor-42768599-97-7GlutaminaseApoptosisantitumorantiproliferativemetabolic stabilityglutamine metabolismROSapoptosisBALB/c SPF nude miceHCT116 cellsInhibitorinhibitorinhibit

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