LAS17 T39906

Product Introduction
Bioactivity


英文名: LAS17

描述: LAS17 is a potent and selective tyrosine-directed irreversible inhibitor for glutathione S-Transferase Pi ( GSTP1 ). LAS17 inhibits GSTP1 activity with an IC 50 of 0.5 μM.

体外活性: 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]. 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.

体内活性: 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]. 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.

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

关键字: LAS 17 | LAS-17

LAS17 T39906信息由TargetMol中国为您提供，如您想了解更多关于LAS17 T39906报价、型号、参数等信息，欢迎来电或留言咨询。

注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途