Fumaratehydratase-IN-1是TCA循环的酶，fumaratehydratase-IN-1的抑制作用能够促进细胞的致癌作用。光亲和标记策略的使用把fumaratehydratase作为一种基本的药理靶点。
CAS：1644060-37-6
分子式：C27H30N2O4
分子量：446.54
纯度：98%
存储：Store at -20°C

Background:

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.