LAS17

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

LAS17 

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

LAS17 Chemical Structure

CAS No. : 2362527-67-9

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生物活性

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].

体外研究
(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].

Shanghai Jinpan Biotech Co Ltd 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.

体内研究
(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].

Shanghai Jinpan Biotech Co Ltd 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.

分子量

359.25

Formula

C15H20Cl2N4O2

CAS 号

2362527-67-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [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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