Drug intelligence / Profile preview

SGC-CK2-1

Development stage
Preclinical
Lead developer
Structural Genomics Consortium
Modality
Small Molecules
Administration
In Vitro/research Use Only; Not Approved For Clinical Administration.
01

Overview

SGC-CK2-1 is a highly potent and selective small molecule inhibitor of casein kinase 2 (CK2), a serine/threonine protein kinase involved in diverse cellular processes including cell survival, proliferation, and inflammation. It binds with equal potency to both catalytic subunits of CK2—CK2α (CSNK2A1) and CK2α' (CSNK2A2)—with nanomolar IC50 values. The compound is ATP competitive and demonstrates exceptional selectivity across the kinome. Developed as a chemical probe by the Structural Genomics Consortium (SGC), it has been used to dissect CK2 biology in various models, including cancer and neuroinflammation research. Unlike less selective CK2 inhibitors such as CX-4945, SGC-CK2-1 exhibits minimal off-target activity against other kinases at relevant concentrations[1][3][4][6][7].

Other names
N-(5-{[3-cyano-7-(cyclopropylamino)pyrazolo[1,5-a]pyrimidin-5-yl]amino}-2-methylphenyl)propanamide
02

Targets

CK2 (Casein kinase II subunit alpha)CSNK2A2 (Casein kinase II subunit alpha prime)DYRK2 (Dual-specificity tyrosine-phosphorylation-regulated kinase 2)

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