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

18 May 2020, Version 2
This content is a preprint and has not undergone peer review at the time of posting.

Abstract

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.

Keywords

kinase
chemical probe
CSNK2A2
dark kinase
small molecule
nanoBRET
CSNK2A1
CK2
IDG

Supplementary materials

Title
Description
Actions
Title
CK2 SI for submission 2
Description
Actions

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