Definition
ChEBI: SGC-CK2-1 is a pyrazolopyrimidine that is pyrazolo[1,5-a]pyrimidine which is substituted at positions 3, 5, and 7 by cyano, (4-methyl-3-propanamidophenyl)nitrilo and cyclopropylnitrilo groups, respectively. It is a potent and selective chemical probe for the pleiotropic kinase CK2. It has a role as an EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor. It is a pyrazolopyrimidine, a nitrile, a secondary amino compound, a substituted aniline, a member of cyclopropanes and a secondary carboxamide.
Biological Activity
SGC-CK2-1 is a highly potent, ATP-competitive, and cell-active CK2 chemical probe with exclusive selectivity for both human CK2 isoforms, with IC50s of 36 and 16 nM for CK2α and CK2α′respectively in the nanoBRET assay. SGC-CK2-1 can be used for the research of neurodegenerative diseases[1][2].
SGC-CK2-1 inhibits CSNK2A2 and CSNK2A1 with IC50s value of 2.3 and 4.2 nM[1].SGC-CK2-1 inhibits DYRK2 with the IC50 value of 3.7 μM[1].SGC-CK2-1 inhibits blood U-937, MV4-11, MOLM-13, OCI-LY19, OCI-AML5 cells with IC50s of 120, 690, 750, 760 and 810 nM, respectively. SGC-CK2-1 inhibits Head/Neck Detroit562 cells with an IC50 of 550 nM. SGC-CK2-1 inhibits Lung NCI-H2286 cells with an IC50 of 550 nM. SGC-CK2-1 inhibits Brain SK-N-MC cells with an IC50 of 730 nM. SGC-CK2-1 inhibits Breast BT-20 cells with an IC50 of 810 nM. SGC-CK2-1 inhibits Skin A375 cells with an IC50 of 830 nM. SGC-CK2-1 inhibits Stomach SNU-1 cells with an IC50 of 860 nM. SGC-CK2-1 inhibits Duodenum Hutu 80 cells with an IC50 of 920 nM[1].
References
[1]. Carrow I Wells, et al. Development of a potent and selective chemical probe for the pleiotropic kinase CK2. Cell Chem Biol. 2021 Apr 15;28(4):546-558.e10. [2]. Marco P Licciardello, et al. A New Chemical Probe Challenges the Broad Cancer Essentiality of CK2. Trends Pharmacol Sci. 2021 May;42(5):313-315.
