A Cell-Permeable Ester Derivative of the JmjC Histone Demethylase Inhibitor IOX1 (pages 566–571)
Rachel Schiller, Dr. Giuseppe Scozzafava, Dr. Anthony Tumber, Dr. James R. Wickens, Jacob T. Bush, Dr. Ganesha Rai, Dr. Clarisse Lejeune, Dr. Hwanho Choi, Dr. Tzu-Lan Yeh, Mun Chiang Chan, Dr. Bryan T. Mott, Dr. James S. O. McCullagh, Dr. David J. Maloney, Prof. Christopher J. Schofield and Dr. Akane Kawamura
Version of Record online: 6 FEB 2014 | DOI: 10.1002/cmdc.201300428
A new tool in epigenetics: Ester derivatives of 5-carboxy-8-hydroxyquinoline (IOX1), a broad-spectrum inhibitor of 2OG oxygenases, including the JmjC demethylases, were evaluated for their in vitro activity against enzymes and in cell-based assays. Results showed a dependence of JmjC inhibition on the aliphatic chain length, with the n-octyl ester showing both enhanced cellular potency (30-fold) and improved selectivity over the parent IOX1.