AP-III-a4 (ENOblock)

製品コードS7443

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)
Ethanol 100 mg/mL (158.43 mM)
Water 9 mg/mL (14.25 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 (ENOblock) 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, it also induces glucose uptake and inhibits phosphoenolpyruvate carboxykinase (PEPCK) expression. [1]
in vivo In a HCT116-xenotransplanted zebrafish tumor xenograft model, AP-III-a4 (ENOblock) (10 μM) inhibits cancer cell migration and invasion processes. In vivo, it 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
Enolase activity 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 AP-III-a4 (ENOblock) or NaF. 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. 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

AP-III-a4 (ENOblock) is used to treat 3 x 105 HCT116 cells seeded in a 6 well plate for 24 h, with or without prior induction of hypoxia for 4 h, using triplicate wells. After 24 h of treatment with this compound, cells are 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 --

参考

  • https://pubmed.ncbi.nlm.nih.gov/23547795/

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：

LncPRESS1 promotes the progression and cisplatin resistance of breast cancer through upregulation of ENO1 and activation of glycolysis [ Cell Div, 2025, 20(1):23] PubMed: 41046264
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
Evolutionary genomics identifies host-directed therapeutics to treat intracellular bacterial infections [ bioRxiv, 2023, 10.1101/2023.08.01.551011] PubMed: None
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

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。

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