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SGC-CK2-1: The First Selective Chemical Probe for the Pleiotropic Kinase CK2
preprintrevised on 15.05.2020, 17:58 and posted on 18.05.2020, 04:46 by Carrow Wells, David Drewry, Julie E. Pickett, Alison D. Axtman
Building upon a wealth of published knowledge surrounding the pyrazolopyrimidine scaffold, we designed a small library around the most selective small molecule CK2 inhibitors reported. Through extensive evaluation of this library we identified inhibitor 24 (SGC-CK2-1) as a potent, selective, and cell-active CK2 chemical probe. Remarkably, despite years of research pointing to CK2 as a key driver in cancer, our probe did not elicit an antiproliferative phenotype in cell lines tested. While many publications have attempted tocharacterize CK2 function, CK2 biology is complex and a high-quality chemical tool like SGC-CK2-1 will aid in connecting CK2 functions to phenotypes.
Eshelman Institute for Innovation
Canada Foundation for Innovation
Innovative Medicines Initiative
Ontario Ministry of Economic Development and Innovation
São Paulo Research Foundation-FAPESP
A UK Hub to Catalyse Open Target Discovery.
Wellcome TrustFind out more...
North Carolina Biotechnology Center
Illuminating Function of the Understudied Druggable Kinome
National Institute of Diabetes and Digestive and Kidney DiseasesFind out more...