AP-III-a4 (ENOblock)

製品コードS7443 バッチS744301

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C31H44ClFN8O3
分子量 631.18 CAS No. 1177827-73-4
Solubility (25°C)* 体外 DMSO 100 mg/mL (158.43 mM)
Water 100 mg/mL (158.43 mM)
Ethanol 100 mg/mL (158.43 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 AP-III-a4 (ENOblock) is the first nonsubstrate analogue inhibitor of enolase with IC50 of 0.576 μM.
in vitro In HCT116 cells, AP-III-a4 induces cell death under hypoxia, and inhibits cancer cell migration and invasion by down-regulation of AKT and Bcl-xL expression. In Huh7 hepatocytes and HEK kidney cells, AP-III-a4 induces glucose uptake and inhibits phosphoenolpyruvate carboxykinase (PEPCK) expression. [1]
in vivo In a HCT116-xenotransplanted zebrafish tumor xenograft model, AP-III-a4 (10 μM) inhibits cancer cell migration and invasion processes. In vivo, AP-III-a4 (10 μM) also causes downregulation of PEPCK expression and induction of glucose uptake, and inhibits adipogenesis and foam cell formation. [1]

プロトコル(参考用のみ)

キナーゼアッセイ Enolase activity assay
A single unit of enolase is defined as the amount of enzyme that produces 1 μmol of phosphoenol pyruvate from phospho-D-glycerate/min in standard assay. Enolase activity assay is measured at 37°C by incubating pure enolase (3–9 U) in a buffer containing 50 mM imidazole-HCl (pH 6.8), 2.0 mM MgSO4 and 400 mM KCl in the absence or presence of ENOblock or NaF. The reaction is initiated by adding 1 μmol of 2-phospho-D-glycerate, and the OD is measured after 10 min of reaction time with a spectrophometer at 240 nm.
細胞アッセイ 細胞株 HCT116 cells
濃度 5 μM
反応時間 24 h
実験の流れ

3 x 105 HCT116 cells are seeded in a 6 well plate. 24 h later, cells are treated with compound of interest (with or without prior induction of hypoxia for 4 h) for 24 h using triplicate wells. Cells are then trypsinized and resuspended in 2.5 mL PBS. A 100 μL aliquot is taken for staining with 0.2% trypan blue solution and counted using a hemocytometer. 150 cells are counted and dead cells are classified as those that could not exclude trypan blue.
動物実験 動物モデル HCT116-xenotransplanted zebrafish tumor xenograft model
投薬量 10 μM
投与方法 --

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Mediation of PKM2-dependent glycolytic and non-glycolytic pathways by ENO2 in head and neck cancer development [ J Exp Clin Cancer Res, 2023, 42(1):1] PubMed: 36588153
A temperature-regulated circuit for feeding behavior [ Nat Commun, 2022, 13(1):4229] PubMed: 35869064
A temperature-regulated circuit for feeding behavior [ Nat Commun, 2022, 13(1):4229] PubMed: 35869064
The essential roles of m6A RNA modification to stimulate ENO1-dependent glycolysis and tumorigenesis in lung adenocarcinoma [ J Exp Clin Cancer Res, 2022, 41(1):36] PubMed: 35078505
Amoxicillin Haptenation of α-Enolase is Modulated by Active Site Occupancy and Acetylation [ Front Pharmacol, 2021, 12:807742] PubMed: 35095517
Preclinical validation of Alpha-Enolase (ENO1) as a novel immunometabolic target in multiple myeloma. [ Oncogene, 2020, 39(13):2786-2796] PubMed: 32024967
FGFRL1 affects chemoresistance of small-cell lung cancer by modulating the PI3K/Akt pathway via ENO1. [ J Cell Mol Med, 2020, 24(3):2123-2134] PubMed: 31957179
The Synergism of the Small Molecule ENOblock and Fluconazole Against Fluconazole-Resistant Candida albicans. [ Front Microbiol, 2019, 10:2071] PubMed: 31555252
Structural and Functional Studies of Bacterial Enolase, a Potential Target Against Gram-Negative Pathogens. [Krucinska J Biochemistry, 2018, 10.1021/acs.biochem.8b01298] PubMed: 30714720

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。