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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C31H44ClFN8O3 |
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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. |
製品説明 | AP-III-a4 (ENOblock) is the first nonsubstrate analogue inhibitor of enolase with IC50 of 0.576 μM. |
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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] |
キナーゼアッセイ | Enolase activity assay | |
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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. |
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動物実験 | 動物モデル | HCT116-xenotransplanted zebrafish tumor xenograft model |
投薬量 | 10 μM | |
投与方法 | -- |
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。
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