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LAS17

CAS No. : 2362527-67-9

MCE 站：LAS17

产品活性：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 ?M.

研究领域：Metabolic Enzyme/Protease

作用靶点：Gutathione S-transferase

In Vitro: Glutathione?S-Transferase Pi (GSTP1) mediates cellular defense against reactive electrophiles. LAS17 inhibits GSTP1 activity?in vitro?in a concentration-dependent manner.?
LAS17 (10 ?M; 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 ?M) 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.

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.

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