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CX-4945 | CX-4945 : ATP competitive inhibitor of CSNK2A1
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (2 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
  • Ki:0.38 nM
  • IC50:1 nM
ATP competitive
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Selectivity

In Vitro Selectivity Assessment

Potency: IC50 - CK2 1 nM, DAPK3 17 nM, FLT3 35 nM, TBK1 35 nM, CLK3 41 nM, HIPK 45 nM, PIM1 46 nM, CDK1 56 nM

Potency Assay Off-Target:
CX-4945 was tested against 285 kinases in Millipore Kinase Profiler, and in vitro kinase assays. In ...

Potency
Cellular
In Vitro

CSNK2A1

Mode of Action: ATP competitive

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1158/0008-5472.CAN-10-1893

In Vivo Validations

Mouse
Dose: 75 mg/mL
Route of delivery: Oral
Systemic clearance: 2.7 L/kg/hr
Organ of interest (O): xenograft
Target engagement assay: Indirect: immunohistochemistry showed inhibition of protein substrate phosphorylation in xenograft tumor tissue (phosphorylation of p21 at T145).

DOI Reference: 10.1158/0008-5472.CAN-10-1893

Orthogonal Probes def

SGC-CK2-1

Chemical Information

Molecular Formula C19H12ClN3O2
SMILEs O=C(O)c1ccc2c(c1)nc(Nc1cccc(Cl)c1)c1ccncc12
InChI InChI=1S/C19H12ClN3O2/c20-12-2-1-3-13(9-12)22-18-15-6-7-21-10-16(15)14-5-4-11(19(24)25)8-17(14)23-18/h1-10H,(H,22,23)(H,24,25)
Molecular weight 349.06 Da
AlogP 4.878200000000002
HBond acceptors 5
HBond donors 2
Atoms 37

References

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Vendors

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Expert Reviews

by SERP
(on 27 Jun 2016 )
Cellular Use Rating
In Model Organisms
CX-4945 is a highly potent inhibitor of CLKs (IC50 range ~ 4-90 nM, top target CLK2 with an IC50 of 3.8 nM), and it therefore exerts a strong and profound effect on pre-mRNA splicing in a CK2-independent...
by SERP
(on 1 Jul 2016 )
Cellular Use Rating
In Model Organisms
CX-4945 should be used with caution due to significant off-target activity; appropriate control experiments should be included. CX-4945 also inhibits DAPK3, FLT3, TBK1, CLK3, HIPK3, PIM1, and CDK1/cyclin...

Portal Comments

Grygier P. et al 2023 publication (DOI: 10.1021/acs.jmedchem.2c01887) shows that Silmitasertib is a dual inhibitor for DYRK1A and GSK3β kinases. "CX-4945 strongly binds to DYRK1A and GSK3β kinases with...

(last updated: 15 Mar 2023)

Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria