LWG-301
Based on 1 publication(s) in Google Scholar
LWG-301 is an allosteric inhibitor of Glutaminase 1 (GLS1) with an IC50 value of 7 nM. LWG-301 significantly block glutamine metabolism, increases intracellular ROS, thus induces apoptosis. LWG-301 exhibits moderate antitumor effects in HCT116 xenograft model.
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- CAS. Nr.: 3038480-88-2
- Formel: C28H38N8O3S
- Molecular Weight:566.72
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Publications Citing Use of MedChemExpress (MCE) LWG-301
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Biologische Aktivität
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
0.061 μM
Compound: 41a; LWG301
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Antiproliferative activity against human HCT-116 cells incubated for 72 hrs by MTT assay
Antiproliferative activity against human HCT-116 cells incubated for 72 hrs by MTT assay
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[PMID: 36525694] |
| HCT-116 | IC50 |
41.47 μM
Compound: 41a; LWG301
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Antiproliferative activity against human HCT-116 cells in presence of alpha-ketoglutarate
Antiproliferative activity against human HCT-116 cells in presence of alpha-ketoglutarate
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[PMID: 36525694] |
LWG-301 (compound 41a) inhibits HCT116 cancer cells growth with an IC50 value of 61 nM[1].
LWG-301 has great metabolic stability in human liver microsomes with T1/2=108 min, CL=32 μL/min/mg[1].
LWG-301 (10 μM; 6 h) interacts with GLS1 protein in a dose- and time-dependent manner[1].
LWG-301 (0.03-3 μM; 14 d) inhibits the colony formation of HCT116 cells in a concentration-dependent manner[1].
LWG-301 (0.2 μM, 1 μM, 5 μM; 24 h) blocks the metabolism of glutamine thus results a decrease of glutamate, glutathione, and fumaric acid[1].
LWG-301 (1-10 μM; 24 h) induces ROS production and (0.1-10 μM; 24 h) induces apoptosis in HCT116 cells[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:0.001, 0.01, 0.1, 1, and 10 μM
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Incubation Time:10, 30, 60, 180, 240 min
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Result:Showed the interaction with GLS1 in a dose- and time-dependent manner.
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Cell Line:HCT116 cells
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Concentration:1, 5, and 10 μM
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Incubation Time:6 hours
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Result:Induced ROS production in HCT116 cells.
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Cell Line:HCT116 cells
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Concentration:0.1, 0.3, 1, 3, and 10 μM
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Incubation Time:24 hours
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Result:Induced apoptosis in HCT116 cells
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:HCT116 tumor-bearing nude mice[1]
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Dosage:100 mg/kg;
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Administration:Intraperitoneal injection; once a day for 20 days;
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Result:Reduced tumor growth, resulting in 38.9% tumor growth inhibition.
Showed little toxicity on main organ.
Chemical Information
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CAS. Nr. 3038480-88-2
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Molecular Weight 566.72
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Formel C28H38N8O3S
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SMILES
CCCCOC1=CC=CC(CC(NC2=NN=C(C=C2)N3CCC(CC3)NC4=NN=C(S4)NC(CCCC)=O)=O)=C1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Journal Impact Factor
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Most Recent
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Cell Death Dis
Fumarate induces LncRNA-MIR4435-2HG to regulate glutamine metabolism remodeling and promote the development of FH-deficient renal cell carcinoma. [Abstract]2024 Feb 19;15(2):151. PMID: 38374146
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Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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