GLS1 Inhibitor-6
GLS1 Inhibitor-6 (Compound 24y) is an orally active, potent and selective glutaminase 1 (GLS1) inhibitor (IC50=68 nM), shows 220-fold selectivity for GLS2. GLS1 Inhibitor-6 shows good anti-tumor activity, antitumor cell proliferation activity and induces apoptosis.
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- CAS No.: 3033615-55-0
- Formule: C37H52N6O3S
- Masse moléculaire:660.91
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
IC50: 68 nM (GLS1)[1]
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Cell Line
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Type | Value | Description | References |
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| A549 | IC50 |
0.57 μM
Compound: 24y
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Antiproliferative activity against human A549 cells assessed as reduction in cell viability
Antiproliferative activity against human A549 cells assessed as reduction in cell viability
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[PMID: 36055003] |
| HCT-116 | IC50 |
0.42 μM
Compound: 24y
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Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability
Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability
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[PMID: 36055003] |
GLS1 Inhibitor-6 (0-10 μM) inhibts cancer cell growth[1].
GLS1 Inhibitor-6 (1-10 μM, 48 h) can induce A549 cell apoptosis[1].
GLS1 Inhibitor-6 (50-800 nM, 48 h) can induce cell cycle arrest in the G1 phase[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549 and HCT116 cell
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Concentration:0-10 μM
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Incubation Time:
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Result:Inhibited A549 and HCT116 cell growth with IC50s of 0.57 and 0.42 μM, respectively.
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Cell Line:A549 cell
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Concentration:1, 5, and 10 μM
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Incubation Time:48 h
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Result:Showed the population of apoptotic cells to 84% at the concentration of 10 μM.
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Cell Line:A549 cell
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Concentration:50, 100, 200, 400 and 800 nM
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Incubation Time:48 h
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Result:Resulted in G1 phase cell cycle arrest in a dose-dependent manner, and decreased proportion of cells in the S phase.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rats[1]
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Dosage:3 mg/kg
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Administration:I.V. and P.O.; 3 mg/kg; once
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Result:
1.19 The pharmacokinetic parameters of GLS1 Inhibitor-5 (compound 24y)[1].
Parameters I.V. P.O. t1/2 (h) 9.9 19.8 CL (L/h/kg) 6.1 33.4 Cmax ng/mL 699.1 41.3 AUC0–t (ng·h/mL) 2092.3 251.6 F% 12.4
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Animal Model:Human non-small cell lung A549 xenograft tumor model, GLS1 high-expression HCT116 xenograft tumor model[1]
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Dosage:100 mg/kg
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Administration:Oral gavage; 100 mg/kg; once daily; 28 days
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Result:Showed 40.9% tumor growth inhibition in A549 model, and showed 42% tumor growth inhibition in HCT116 model.
Chemical Information
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CAS No. 3033615-55-0
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Masse moléculaire 660.91
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Formule C37H52N6O3S
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SMILES
O=C(NCC1CCN(CCCCCC)CC1)C2=CC=CC(COCCC3CCN(C4=NN=C(NC(CC5=CC=CC=C5)=O)S4)CC3)=C2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
GLS1 Inhibitor-6 Related Classifications
HY-151434 Related Classifications
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