Related Experiment Video
Updated: Aug 7, 2026
11:11
Identification of Novel CK2 Kinase Substrates Using a Versatile Biochemical Approach
Published on: February 21, 2019
CK2 Chemical Probes: Past, Present, and Future
Han Wee Ong1, David H Drewry1,2, Alison D Axtman1
1Structural Genomics Consortium, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA.
Kinases and Phosphatases
|August 6, 2026
Summary
This review summarizes small molecule inhibitors of casein kinase 2 (CK2/CSNK2), focusing on pyrazolo[1,5-a]pyrimidines and naphthyridines. It highlights the utility of SGC-CK2-1 and proposes criteria for ideal in vivo CK2 chemical probes.
Area of Science:
- Biochemistry
- Medicinal Chemistry
- Pharmacology
Background:
- Casein kinase 2 (CK2/CSNK2) is a crucial kinase implicated in numerous cellular functions.
- Its role in various diseases makes CK2 a significant therapeutic target.
- Developing selective CK2 inhibitors and chemical probes is a key research area.
Purpose of the Study:
- To review existing small molecule inhibitors of CK2.
- To discuss different classes of CK2 inhibitors, including orthosteric, allosteric, and bivalent compounds.
- To highlight the development and application of pyrazolo[1,5-a]pyrimidine and naphthyridine chemotypes for CK2 research.
Main Methods:
- Literature review of small molecule inhibitors targeting CK2.
- Analysis of different inhibitor classes and their mechanisms.
- Focus on pyrazolo[1,5-a]pyrimidines and naphthyridines for chemical probe development.
- Evaluation of the chemical probe SGC-CK2-1's utility in cellular studies.
Main Results:
- Various small molecule inhibitors for CK2 have been reported, including orthosteric, allosteric, and bivalent types.
- Pyrazolo[1,5-a]pyrimidines and naphthyridines are promising chemotypes for CK2 probe development.
- The pyrazolo[1,5-a]pyrimidine probe SGC-CK2-1 has been adopted and utilized in cellular research.
Conclusions:
- While SGC-CK2-1 shows utility, no current chemical probe fully meets the criteria for in vivo CK2 investigation.
- Further research is needed to develop ideal in vivo chemical probes for CK2.
- Future directions focus on advancing CK2 inhibitor and probe development for in vivo applications.
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