{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"submitter":["Davis-Gilbert ZW"],"funding":["Innovative Medicines Initiative","Cancer Research UK","Eshelman Institute for Innovation, University of North Carolina","NIDDK NIH HHS","Fondation Leducq","Funda??o Amaz?nia Paraense de Amparo ? Pesquisa","U.S. Department of Defense","Canada Foundation for Innovation","National Institutes of Health","North Carolina Biotechnology Center","Genome Canada","Ontario Genomics Institute"],"pagination":["432-441"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC10108397"],"repository":["biostudies-literature"],"omics_type":["Unknown"],"volume":["14(4)"],"pubmed_abstract":["Naphthyridine-based inhibitors were synthesized to yield a potent and cell-active inhibitor of casein kinase 2 (CK2). Compound <b>2</b> selectively inhibits CK2α and CK2α' when profiled broadly, thereby making it an exquisitely selective chemical probe for CK2. A negative control that is structurally related but lacks a key hinge-binding nitrogen (<b>7</b>) was designed on the basis of structural studies. Compound <b>7</b> does not bind CK2α or CK2α' in cells and demonstrates excellent kinome-wide selectivity. Differential anticancer activity was observed when compound <b>2</b> was profiled alongside a structurally distinct CK2 chemical probe: SGC-CK2-1. This naphthyridine-based chemical probe (<b>2</b>) represents one of the best available small molecule tools with which to interrogate bi"],"journal":["ACS medicinal chemistry letters"],"pubmed_title":["Discovery of a Potent and Selective Naphthyridine-Based Chemical Probe for Casein Kinase 2."],"pmcid":["PMC10108397"],"funding_grant_id":["U24DK116204","AL190107","U24 DK116204","2018-IDG-1030"],"pubmed_authors":["Dunford JE","Havener TM","Oppermann U","Drewry DH","Wells CI","Axtman AD","Howell S","Bashore FM","Hossain MA","Kramer A","Smith JL","Senbabaoglu F","Davis-Gilbert ZW"],"additional_accession":[]},"is_claimable":false,"name":"Discovery of a Potent and Selective Naphthyridine-Based Chemical Probe for Casein Kinase 2.","description":"Naphthyridine-based inhibitors were synthesized to yield a potent and cell-active inhibitor of casein kinase 2 (CK2). Compound <b>2</b> selectively inhibits CK2α and CK2α' when profiled broadly, thereby making it an exquisitely selective chemical probe for CK2. A negative control that is structurally related but lacks a key hinge-binding nitrogen (<b>7</b>) was designed on the basis of structural studies. Compound <b>7</b> does not bind CK2α or CK2α' in cells and demonstrates excellent kinome-wide selectivity. Differential anticancer activity was observed when compound <b>2</b> was profiled alongside a structurally distinct CK2 chemical probe: SGC-CK2-1. This naphthyridine-based chemical probe (<b>2</b>) represents one of the best available small molecule tools with which to interrogate bi","dates":{"release":"2023-01-01T00:00:00Z","publication":"2023 Apr","modification":"2026-05-29T03:36:32.678Z","creation":"2025-04-06T19:10:48.018Z"},"accession":"S-EPMC10108397","cross_references":{"pubmed":["37077385"],"doi":["10.1021/acsmedchemlett.2c00530"]}}