GLS1 Inhibitor-4

Name: GLS1 Inhibitor-4
Brand: MedChemExpress
SKU: HY-146617

Cat. No.: HY-146617: FAQs
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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

CAS No. : 2768599-97-7

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Description

IC₅₀ & Target

IC₅₀: 11.86 nM (GLS1)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
CT26	IC₅₀	0.32 μM Compound: 41e	Antiproliferative activity against mouse CT26 cells overexpressing GLS1 assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against mouse CT26 cells overexpressing GLS1 assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 35428013]
H22	IC₅₀	10.84 μM Compound: 41e	Antiproliferative activity against mouse H22 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against mouse H22 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 35428013]
HCT-116	IC₅₀	0.051 μM Compound: 41e	Antiproliferative activity against human HCT-116 cells overexpressing GLS1 assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against human HCT-116 cells overexpressing GLS1 assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 35428013]
MDA-MB-436	IC₅₀	0.37 μM Compound: 41e	Antiproliferative activity against human MDA-MB-436 cells overexpressing GLS1 assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-436 cells overexpressing GLS1 assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 35428013]

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 (K_d) 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.

2768599-97-7

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

Handling Instructions (2659 KB)

References

[1]. Xu X, et al. Discovery of novel glutaminase 1 allosteric inhibitor with 4-piperidinamine linker and aromatic heterocycles. Eur J Med Chem. 2022 Jun 5;236:114337. [Content Brief]

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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