1438071-28-3Relevant articles and documents
Optimized chemical probes for REV-ERBα
Trump, Ryan P.,Bresciani, Stefano,Cooper, Anthony W. J.,Tellam, James P.,Wojno, Justyna,Blaikley, John,Orband-Miller, Lisa A.,Kashatus, Jennifer A.,Boudjelal, Mohamed,Dawson, Helen C.,Loudon, Andrew,Ray, David,Grant, Daniel,Farrow, Stuart N.,Willson, Timothy M.,Tomkinson, Nicholas C. O.
, p. 4729 - 4737 (2013)
REV-ERBα has emerged as an important target for regulation of circadian rhythm and its associated physiology. Herein, we report on the optimization of a series of REV-ERBα agonists based on GSK4112 (1) for potency, selectivity, and bioavailability.(1) Potent REV-ERBα agonists 4, 10, 16, and 23 are detailed for their ability to suppress BMAL and IL-6 expression from human cells while also demonstrating excellent selectivity over LXRα. Amine 4 demonstrated in vivo bioavailability after either iv or oral dosing.
