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LAS17

Catalog No. T39906 CAS 2362527-67-9

Synonyms: LAS17

LAS17, a potent and selective irreversible inhibitor targeting tyrosine in glutathione S-Transferase Pi (GSTP1), effectively inhibits GSTP1 activity, demonstrated by an IC50 value of 0.5 μM.

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LAS17, CAS 2362527-67-9

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Description	LAS17, a potent and selective irreversible inhibitor targeting tyrosine in glutathione S-Transferase Pi (GSTP1), effectively inhibits GSTP1 activity, demonstrated by an IC50 value of 0.5 μM.
In vitro	Glutathione S-Transferase Pi (GSTP1) plays a crucial role in cellular defense by detoxifying reactive electrophiles. LAS17 is identified to inhibit GSTP1 function in a dose-dependent manner in vitro. At a concentration of 10 μM and after 48 hours of serum-free incubation, LAS17 treatment in 231MFP breast cancer cells mirrors the cell survival challenges witnessed with GSTP1 genetic inactivation. Furthermore, treating 231MFP cells with LAS17 at the same concentration results in heightened phosphorylation of AMPK and acetyl CoA carboxylase (ACC), alongside diminished levels of ATP, lactic acid, purine nucleotides, and certain lipid classes, with an increase in acyl carnitines (ACs), ceramides, and lysophospholipids. Cell viability assays and Western blot analysis conducted under these conditions confirmed the recapitulation of serum-free cell survival impairments and the observed biochemical alterations, underscoring LAS17's potential to mimic GSTP1 inhibition effects.
In vivo	Administering LAS17 daily at a dosage of 20 mg/kg intraperitoneally (prepared in PBS:ethanol:PEG40 (18:1:1)) notably inhibits the growth of 231MFP breast tumor xenografts in severe combined immunodeficiency (SCID) mice. Initiating treatment 2 days post-subcutaneous cell injection significantly restricts tumor expansion and even when begun 16 days after tumor implantation, LAS17 still effectively decelerates tumor progression. This intervention exhibits no observable toxicity or weight change in the mice[2].

Synonyms	LAS17
Molecular Weight	359.25
Formula	C15H20Cl2N4O2
CAS No.	2362527-67-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

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. 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.

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Keywords

LAS17 2362527-67-9 LAS 17 LAS-17 inhibitor inhibit

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