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Art. -Nr.: HY-115673

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LAS17

1 Cited Publications

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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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Reinheit: 97.46%
CAS. Nr.: 2362527-67-9
Formel: C₁₅H₂₀Cl₂N₄O₂
Molecular Weight:359.25

Speicherung:

Pure form -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

LAS17 Chemical Structure

CAS. Nr.: 2362527-67-9

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Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

LAS17 is a potent and selective tyrosine-directed irreversible inhibitor for glutathione S-Transferase Pi (GSTP1) ^[1]. LAS17 inhibits GSTP1 activity with an IC₅₀ of 0.5 μM^[2]. 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.

In Vitro

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.

Cell Viability Assay^[2]

Cell Line:

231MFP breast cancer cells
Concentration:

10 µM
Incubation Time:

48 hours
Result:

Recapitulated the serum-free cell survival impairments observed with genetic inactivation of GSTP1.

Western Blot Analysis^[2]

Cell Line:

231MFP cells
Concentration:

10 µM
Incubation Time:
Result:

LAS17-treated 231MFP cells show increased levels of phosphorylated AMPK and ACC.

In Vivo

Daily administration of LAS17 (20 mg/kg ip, once per day) significantly impairs 231MFP breast tumor xenograft growth in immune-deficient mice when treatment is initiated 2 days after subcutaneous injection of cells, and LAS17 even slows tumor growth when initiated 16 days after tumor implantation, with no observable toxicity and no weight-change^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Severe combined immunodeficiency (SCID) mice bearing 231MFP tumor xenograft^[2]
Dosage:

20 mg/kg (prepared in PBS:ethanol:PEG40 (18:1:1))
Administration:

Daily administration i.p., once per day
Result:

Significantly impaired 231MFP breast tumor xenograft growth.

Chemical Information

CAS. Nr. 2362527-67-9
Appearance Oil
Molecular Weight 359.25
Formel C₁₅H₂₀Cl₂N₄O₂
Color Colorless to light yellow
SMILES

CC(C)C[C@H](C(OC)=O)N(C1=NC(Cl)=NC(Cl)=N1)CCCC#C
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

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

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.7836 mL

13.9179 mL

27.8358 mL

5 mM

0.5567 mL

2.7836 mL

5.5672 mL

10 mM

0.2784 mL

1.3918 mL

2.7836 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

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MOQ

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100 mg

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Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise

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LAS17

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Covalent Screening Library

Anti-Breast Cancer Compound Library

Cuproptosis Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Bioactive Compound Library

Amino Acid Metabolism Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Alkyne Compound Library

Publications Citing Use of MedChemExpress (MCE) LAS17

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

LAS17

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Covalent Screening Library

Anti-Breast Cancer Compound Library

Cuproptosis Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Bioactive Compound Library

Amino Acid Metabolism Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Alkyne Compound Library

Publications Citing Use of MedChemExpress (MCE) LAS17

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

LAS17 Related Classifications

HY-115673 Related Classifications