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SGC-CK2-1: The First Selective Chemical Probe for the Pleiotropic Kinase CK2

preprint
revised on 15.05.2020 and posted on 18.05.2020 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.

Funding

Eshelman Institute for Innovation

Canada Foundation for Innovation

Genome Canada

Innovative Medicines Initiative

Ontario Ministry of Economic Development and Innovation

São Paulo Research Foundation-FAPESP

A UK Hub to Catalyse Open Target Discovery.

Wellcome Trust

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North Carolina Biotechnology Center

Illuminating Function of the Understudied Druggable Kinome

National Institute of Diabetes and Digestive and Kidney Diseases

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History

Email Address of Submitting Author

Alison.Axtman@unc.edu

Institution

University of North Carolina at Chapel Hill

Country

United States

ORCID For Submitting Author

0000-0003-4779-9932

Declaration of Conflict of Interest

The authors declare no competing financial interest.

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