AP-III-a4 (ENOblock)

製品コードS7443

化学情報

	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


* <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) は、0.576 μM の IC50 を持つ、エノラーゼの最初の非基質アナログ阻害剤です。
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.
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.

プロトコル(参考用のみ)

キナーゼアッセイ	Enolase activity assay
キナーゼアッセイ	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
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。

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