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SGC-CK2-2 | SGC-CK2-2 : Inhibitor of CSNK2A1, 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

Targets Biochemical/Biophysical Potency Cellular Potency
CSNK2A1
  • IC50:3.0 nM
  • IC50:920 nM
CSNK2A2
  • IC50:<1.0 nM
  • IC50:200 nM
Inhibitor
up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
SGC-CK2-2 was profiled in the KINOMEscan assay against 403 wild-type kinases at 1 μM. Only 3 kinases ...

Potency
Cellular
In Vitro

CSNK2A1

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acsmedchemlett.2c00530

CSNK2A2

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acsmedchemlett.2c00530

Negative Control Compounds

SGC-CK2-2N
Notes: cpd 7 was evaluated in NanoBRET and found not to bind either target up to 10 uM
SMILES: OC(C1=CC2=NC(NCC3=CC=CC=C3)=C4N=CC=CC4=C2C=C1)=O

Orthogonal Probes def

SGC-CK2-1
SILMITASERTIB

Chemical Information

Molecular Formula C19H14N4O2
SMILEs O=C(O)c1ccc2c(c1)nc(NCc1ccccc1)c1ncncc12
InChI InChI=1S/C19H14N4O2/c24-19(25)13-6-7-14-15-10-20-11-22-17(15)18(23-16(14)8-13)21-9-12-4-2-1-3-5-12/h1-8,10-11H,9H2,(H,21,23)(H,24,25)
Molecular weight 330.11 Da
AlogP 0.0
HBond acceptors 6
HBond donors 2
Atoms 39

Expert Reviews

by SERP
(on 9 Jun 2023 )
Cellular Use Rating
Given the lack of proteome-wide profiling, unknown non-kinase targets cannot be excluded.
by SERP+
(on 17 Jun 2024 )
Cellular Use Rating
Not recommended for cellular work since this compound showed poor activity for inhibiting AKT phosphorylation. NanoBRET showed inconsistent IC50 with enzymatic assay.
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