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SGC-CK2-1 | SGC-CK2-1 : ATP competitive inhibitor of CSNK2A1 and CSNK2A2
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

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Targets Biochemical/Biophysical Potency Cellular Potency
CSNK2A1
  • IC 50:4.2 nM @ 10µM ATP
  • IC 50:36 nM
CSNK2A2
  • IC 50:2.3 nM @ 10µM ATP
  • IC 50:16 nM
up to 500 nM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
KINOMEscan
Selectivity Assessment Description:
SGC-CK2-1 was profiled in the KINOMEscan assay against 403 wild-type kinases at 1 μM. Only 11 kinase ...
In Cell Selectivity Assessment
Selectivity Assessment Description:
SGC-CK2-1 was profiled against 140 cancer cell lines in an eight-point dose-response. It inhibited c ...

Potency
Cellular
In Vitro

CSNK2A1

Mode of Action: ATP competitive

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1016/j.chembiol.2020.12.013

CSNK2A2

Mode of Action: ATP competitive

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1016/j.chembiol.2020.12.013

Negative Control Compounds

SGC-CK2-1N
Notes: SGC-CK2-1N was profiled in the KINOMEscan assay against 403 wild-type kinases at 1 μM and follow-up CK2α and CK2α' enzymatic assays were done to confirm no activity.
SMILES: CC1=CC=C(N(C)C2=NC3=C(C#N)C=NN3C(NC4CC4)=C2)C=C1N(C)C(C5CC5)=O

Orthogonal Probes def

SILMITASERTIB

Chemical Information

Molecular Formula C20H21N7O
SMILEs CCC(=O)Nc1cc(Nc2cc(NC3CC3)n3ncc(C#N)c3n2)ccc1C
InChI InChI=1S/C20H21N7O/c1-3-19(28)25-16-8-15(5-4-12(16)2)23-17-9-18(24-14-6-7-14)27-20(26-17)13(10-21)11-22-27/h4-5,8-9,11,14,24H,3,6-7H2,1-2H3,(H,23,26)(H,25,28)
Molecular weight 375.18 Da
AlogP 3.575800000000002
HBond acceptors 8
HBond donors 3
Atoms 49

References

Publications

Cross References

ChEMBL BindingDB PDB PubChem ChEBI canSAR SGC

Expert Reviews

by SERP
(on 20 May 2021)
Cellular Use Rating
There is a disconnect in the linked publication between the NanoBret cellular IC50 of 16-36 nM and the apparent functional IC50 of inhibiting AKT S129 phosphorylation that appears to be ~500 nM. It...
by SERP
(on 20 May 2021)
Cellular Use Rating
SGC-CK2-1 is a valuable probe for interrogating the cellular effects of CK2 inhibition, as it is considerably more selective against related kinases such as DYRK2 than previously reported inhibitors...
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