LAS17

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

LAS17 是一种强效的，不可逆的，选择性谷胱甘肽 S-转移酶 Pi (GSTP1) 抑制剂。LAS17 抑制 GSTP1 活性，IC50 为 0.5 μM.LAS17 是一种点击化学试剂。它含有 Alkyne 基团，可以和含有 Azide 基团的分子发生铜催化的叠氮-炔环加成反应 (CuAAc)。

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.

Glutathione?S-Transferase Pi (GSTP1) mediates cellular defense against reactive electrophiles. LAS17 inhibits GSTP1 activity?in vitro?in a concentration-dependent manner.?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.? GSTP1 knockdown in LAS17 (10 μM) treatment in 231MFP cells results in increased levels of phosphorylated AMPK and acetyl CoA carboxylase (ACC).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 Cell Viability Assay 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 Cell Line:231MFP cells Concentration:10 μM Incubation Time:Result:LAS17-treated?231MFP cells show increased levels of phosphorylated AMPK and ACC.

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.Animal Model:Severe combined immunodeficiency (SCID) mice bearing 231MFP tumor xenograft 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.

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Others

Other Targets

Glutathione Peroxidase

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2362527-67-9

359.25

C15H20Cl2N4O2

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 100 mg/mL (278.36 mM; 超声助溶 )

N([C@@H](C(OC)=O)CC(C)C)(CCCC#C)C=1N=C(Cl)N=C(Cl)N1

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(-20℃)

With Ice Pack

≥ 2 years