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.
| 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 anIC50of 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].
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. |
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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].
| 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Pure form | -20°C | 3 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(278.36 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.7836 mL | 13.9179 mL | 27.8358 mL | | 5 mM | 0.5567 mL | 2.7836 mL | 5.5672 mL | | 10 mM | 0.2784 mL | 1.3918 mL | 2.7836 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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