Fumarate hydratase-IN-1 |
| Catalog No.GC32878 |
La fumarato hidratasa-IN-1 (compuesto 2) es un inhibidor de la fumarato hidratasa permeable a las células. La fumarato hidratasa-IN-1 tiene actividad antiproliferativa contra varias lÍneas celulares de cÁncer con una IC50 media de 2,2 μM.
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Cas No.: 1644060-37-6
Sample solution is provided at 25 µL, 10mM.
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Fumarate hydratase-IN-1, an enzyme of the TCA cycle. Inhibition of fumarate hydratase-IN-1 can contribute to tumorigenicity in some cells. The use of a photoaffinity labeling strategy identified fumarate hydratase as the principal pharmacological target.[1]In vitro: The activity of this enzyme was measured using a well-established assay that monitored the conversion of fumarate into L-malate and subsequent oxidation of L-malate to oxaloacetate by malate dehydrogenase. Initial controls established that neither the carboxylic acid 3 nor ester 2 inhibited malate dehydrogenase Using this two-enzyme protocol we found that carboxylic acid 3 inhibited fumarate hydratase in a dose-dependent fashion in vitro. Besides, inhibition of fumarate hydratase can contribute to tumorigenicity in some cells.[1]
[1]. Takeuchi T et al. Identification of Fumarate Hydratase Inhibitors with Nutrient-Dependent Cytotoxicity. J Am Chem Soc, 2015 Jan 21, 137(2): 564-567.
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