A cell??permeable ester derivative of the JmjC histone demethylase inhibitor IOX1

R Schiller, G Scozzafava, A Tumber…

Index: Schiller, Rachel; Scozzafava, Giuseppe; Tumber, Anthony; Wickens, James R.; Bush, Jacob T.; Rai, Ganesha; Lejeune, Clarisse; Choi, Hwanho; Yeh, Tzu-Lan; Chan, Mun Chiang; Mott, Bryan T.; McCullagh, James S. O.; Maloney, David J.; Schofield, Christopher J.; Kawamura, Akane ChemMedChem, 2014 , vol. 9, # 3 p. 566 - 571

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Citation Number: 13

Abstract

Abstract The 2-oxoglutarate (2OG)-dependent Jumonji C domain (JmjC) family is the largest family of histone lysine demethylases. There is interest in developing small-molecule probes that modulate JmjC activity to investigate their biological roles. 5-Carboxy-8- hydroxyquinoline (IOX1) is the most potent broad-spectrum inhibitor of 2OG oxygenases, including the JmjC demethylases, reported to date; however, it suffers from low cell ...