GLS1 Inhibitor-1
Based on 1 Customer Validation
GLS1 Inhibitor-1 is an orally active, allosteric, selective GLS1 inhibitor with an IC50 of 0.021 µM for GLS1 and an IC50 of 0.051 µM for the GLS1 GAC splice variant. GLS1 Inhibitor-1 increases glutamine and decreases glutamate and aspartate. GLS1 Inhibitor-1 exhibits anticancer activity against non-small cell lung cancer. GLS1 Inhibitor-1 can be used for research on non-small cell lung cancer.
For research use only. We do not sell to patients.
- Purity : 99.61%
- CAS No.: 1832646-52-2
- Formula: C19H21N7O2S
- Molecular Weight:411.48
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Storage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
IC50: 0.021 μM (GLS1)
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| PC-3 | IC50 |
0.0003 μM
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Inhibition of GLS mode of action in human PC-3 cells with IC50 0.0003 μM.
Inhibition of GLS mode of action in human PC-3 cells with IC50 0.0003 μM.
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31199640 |
| NCI-H1703 | GI50 |
0.011 μM
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Inhibition of human NCI-H1703 cell proliferation with GI50 0.011 μM.
Inhibition of human NCI-H1703 cell proliferation with GI50 0.011 μM.
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31199640 |
| CHO | IC50 |
33.3 μM
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Inhibition of hERG channel in Chinese hamster ovary cells with IC50 > 33.3 μM measured using IonWorks HT technology platform.
Inhibition of hERG channel in Chinese hamster ovary cells with IC50 > 33.3 μM measured using IonWorks HT technology platform.
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31199640 |
In Vitro
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SCID (male; Charles River Laboratories; NCI-H1703 subcutaneous xenograft)[1]
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Dosage:100 mg/kg
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Administration:p.o. (oral gavage); once daily; 21 days
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Result:Inhibited tumor growth by 37% by day 21.
Achieved maximum tumor growth inhibition of 73% on day 12.
Doubled tumor glutamine levels relative to control at 4 h and 24 h on day 21.
Reduced tumor glutamate and aspartate levels relative to control on day 21.
Achieved mean concentration of 3.57 μM at 4 h and 3.63 μM at 24 h after oral dosing.
Achieved mean free concentration of 0.582 μM at 4 h and 0.592 μM at 24 h, corresponding to 53-fold and 54-fold free cover over cell GI50.
Chemical Information
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CAS No. 1832646-52-2
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Appearance Solid
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Molecular Weight 411.48
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Formula C19H21N7O2S
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Color White to light yellow
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SMILES
O=C([C@H](C1=CC=CC=C1)OC)NC2=NN=C(S2)N[C@H]3CN(C4=CC=CN=N4)CC3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
In Vitro:
DMSO : 20 mg/mL (48.61 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (284 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4303 mL | 12.1513 mL | 24.3025 mL | 60.7563 mL |
| 5 mM | 0.4861 mL | 2.4303 mL | 4.8605 mL | 12.1513 mL | |
| 10 mM | 0.2430 mL | 1.2151 mL | 2.4303 mL | 6.0756 mL | |
| 15 mM | 0.1620 mL | 0.8101 mL | 1.6202 mL | 4.0504 mL | |
| 20 mM | 0.1215 mL | 0.6076 mL | 1.2151 mL | 3.0378 mL | |
| 25 mM | 0.0972 mL | 0.4861 mL | 0.9721 mL | 2.4303 mL | |
| 30 mM | 0.0810 mL | 0.4050 mL | 0.8101 mL | 2.0252 mL | |
| 40 mM | 0.0608 mL | 0.3038 mL | 0.6076 mL | 1.5189 mL |
GLS1 Inhibitor-1 Related Classifications
HY-136704 Related Classifications
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