Fumarate hydratase-IN-1

Names

[ Name ]:
Fumarate hydratase-IN-1

[Synonym ]:
Ethyl (3S,3aR)-1-(4-biphenylylmethyl)-3-[2-(methylamino)-2-oxoethyl]-2-oxo-1,2,3,4,5,6-hexahydro-3aH-indole-3a-carboxylate
3aH-Indole-3a-carboxylic acid, 1-([1,1'-biphenyl]-4-ylmethyl)-1,2,3,4,5,6-hexahydro-3-[2-(methylamino)-2-oxoethyl]-2-oxo-, ethyl ester, (3S,3aR)-

Biological Activity

[Description]:

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]

[Related Catalog]:

Signaling Pathways >> Others >> Others

Research Areas >> Cancer

[References]

[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.

[Related Small Molecules]

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
693.0±55.0 °C at 760 mmHg

[ Molecular Formula ]:
C₂₇H₃₀N₂O₄

[ Molecular Weight ]:
446.538

[ Flash Point ]:
372.9±31.5 °C

[ Exact Mass ]:
446.220551

[ LogP ]:
4.77

[ Vapour Pressure ]:
0.0±2.2 mmHg at 25°C

[ Index of Refraction ]:
1.616

[ Storage condition ]:
2-8℃

Related Compounds

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