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.
- CAS No.: 2768599-97-7
- Formula: C29H27F3N10O2S2
- Molecular Weight:668.72
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
IC50: 11.86 nM (GLS1)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CT26 | IC50 |
0.32 μM
Compound: 41e
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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
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[PMID: 35428013] |
| H22 | IC50 |
10.84 μM
Compound: 41e
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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
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[PMID: 35428013] |
| HCT-116 | IC50 |
0.051 μM
Compound: 41e
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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
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[PMID: 35428013] |
| MDA-MB-436 | IC50 |
0.37 μM
Compound: 41e
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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
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[PMID: 35428013] |
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.
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Cell Line:HCT116 cells
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Concentration:30, 50, 200 nM
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Incubation Time:24 h
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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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Six-week-old BALB/c SPF nude mice (HCT116 tumor nude mouse xenograft model)[1]
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Dosage:50, 100 mg/kg
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Administration:I.p.; twice a day for 21 consecutive days
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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.
Chemical Information
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CAS No. 2768599-97-7
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Molecular Weight 668.72
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Formula C29H27F3N10O2S2
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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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
GLS1 Inhibitor-4 Related Classifications
HY-146617 Related Classifications
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