CK2-IN-7 (compound 2) is an inhibitor of casein kinase 2 (CK2). CK2-IN-7 shows synergistic effect with structurally distinct CK2 chemical probe: SGC-CK2-1, against cancer[1].
Biological Activity
SGC-CK2-2 is a highly potent and selective casein kinase 2 (CK2CKII) inhibitor (IC50 = 3 nM/CK2α and <1 nM/CK2α by enzyme assay; CK2α/CK2αμ IC50 = 920/200 nM by cellular NanoBRET; genomewide by DiscoverX scanMAX panel at 1 μM). SGC-CK2-2 effectively inhibits CK2 downstream signaling in MDA-MB-231 cells (AKT pS129 IC50 ~5 μM post 24h) without cytotoxicity (up to 10 μM & 48h).
References
[1] Davis-Gilbert ZW, et al. Discovery of a Potent and Selective Naphthyridine-Based Chemical Probe for Casein Kinase 2. ACS Med Chem Lett. 2023 Mar 14;14(4):432-441. DOI:10.1021/acsmedchemlett.2c00530
