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SGC-CK2-1

Names

[ CAS No. ]:
2470424-39-4

[ Name ]:
SGC-CK2-1

Biological Activity

[Description]:

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].

[Related Catalog]:

Signaling Pathways >> Cell Cycle/DNA Damage >> Casein Kinase
Research Areas >> Neurological Disease
Signaling Pathways >> Stem Cell/Wnt >> Casein Kinase

[Target]

CK2α:36 nM (IC50)

CK2α':16 nM (IC50)


[In Vitro]

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.

Chemical & Physical Properties

[ Molecular Formula ]:
C20H21N7O

[ Molecular Weight ]:
375.43


Related Compounds

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