LAS17
Based on 1 publication(s) in Google Scholar
LAS17 is a potent and selective tyrosine-directed irreversible inhibitor for glutathione S-Transferase Pi (GSTP1) . LAS17 inhibits GSTP1 activity with an IC50 of 0.5 μM. LAS17 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- Pureza: 97.46%
- No. CAS: 2362527-67-9
- Fòrmula: C15H20Cl2N4O2
- Peso molecular:359.25
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Almacenamiento:Pure form -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Publications Citing Use of MedChemExpress (MCE) LAS17
More
Actividad biológica
Glutathione S-Transferase Pi (GSTP1) mediates cellular defense against reactive electrophiles. LAS17 inhibits GSTP1 activity in vitro in a concentration-dependent manner[1].
LAS17 (10 μM; Serum-free survival 48 h) treatment in 231MFP breast cancer cells recapitulates the serum-free cell survival impairments observed with genetic inactivation of GSTP1[2].
GSTP1 knockdown in LAS17 (10 μM) treatment in 231MFP cells results in increased levels of phosphorylated AMPK and acetyl CoA carboxylase (ACC)[2].
LAS17 treatment in 231MFP cells also shows reduced levels of ATP, lactic acid, purine nucleotides, and diacylated phospholipids and alkylacyl ether lipids and increased levels of acyl carnitines (ACs), ceramides, lysophospholipids[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:231MFP breast cancer cells
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Concentration:10 µM
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Incubation Time:48 hours
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Result:Recapitulated the serum-free cell survival impairments observed with genetic inactivation of GSTP1.
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Cell Line:231MFP cells
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Concentration:10 µM
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Incubation Time:
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Result:LAS17-treated 231MFP cells show increased levels of phosphorylated AMPK and ACC.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Severe combined immunodeficiency (SCID) mice bearing 231MFP tumor xenograft[2]
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Dosage:20 mg/kg (prepared in PBS:ethanol:PEG40 (18:1:1))
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Administration:Daily administration i.p., once per day
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Result:Significantly impaired 231MFP breast tumor xenograft growth.
Chemical Information
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No. CAS 2362527-67-9
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Appearance Oil
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Peso molecular 359.25
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Fòrmula C15H20Cl2N4O2
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Color Colorless to light yellow
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SMILES
CC(C)C[C@H](C(OC)=O)N(C1=NC(Cl)=NC(Cl)=N1)CCCC#C
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Pure form -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Mol Cell
SMURF2 predisposes cancer cell toward ferroptosis in GPX4-independent manners by promoting GSTP1 degradation. [Abstract]2023 Dec 7;83(23):4352-4369.e8. PMID: 38016474
Solvente y solubilidad
DMSO : 100 mg/mL (278.36 mM; Need ultrasonic; 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. 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. 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)
Pureza y Documentación
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Ficha de datos (277 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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Instrucciones de manejo (2659 KB)
Referencias
[1]. L A Crawford, et al. A tyrosine-reactive irreversible inhibitor for glutathione S-transferase Pi (GSTP1). Mol Biosyst. 2016 May 24;12(6):1768-71. [Content Brief]
[2]. Sharon M Louie, et al. GSTP1 Is a Driver of Triple-Negative Breast Cancer Cell Metabolism and Pathogenicity. Cell Chem Biol. 2016 May 19;23(5):567-578. [Content Brief]
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. 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 | 2.7836 mL | 13.9179 mL | 27.8358 mL | 69.5894 mL |
| 5 mM | 0.5567 mL | 2.7836 mL | 5.5672 mL | 13.9179 mL | |
| 10 mM | 0.2784 mL | 1.3918 mL | 2.7836 mL | 6.9589 mL | |
| 15 mM | 0.1856 mL | 0.9279 mL | 1.8557 mL | 4.6393 mL | |
| 20 mM | 0.1392 mL | 0.6959 mL | 1.3918 mL | 3.4795 mL | |
| 25 mM | 0.1113 mL | 0.5567 mL | 1.1134 mL | 2.7836 mL | |
| 30 mM | 0.0928 mL | 0.4639 mL | 0.9279 mL | 2.3196 mL | |
| 40 mM | 0.0696 mL | 0.3479 mL | 0.6959 mL | 1.7397 mL | |
| 50 mM | 0.0557 mL | 0.2784 mL | 0.5567 mL | 1.3918 mL | |
| 60 mM | 0.0464 mL | 0.2320 mL | 0.4639 mL | 1.1598 mL | |
| 80 mM | 0.0348 mL | 0.1740 mL | 0.3479 mL | 0.8699 mL | |
| 100 mM | 0.0278 mL | 0.1392 mL | 0.2784 mL | 0.6959 mL |
LAS17 Related Classifications
HY-115673 Related Classifications
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