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KH-CB19 | Inhibitor of CLK1, CLK4, DYRK1A
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (1 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
CLK1
  • IC50:19.7 nM
CLK4
  • IC50:530 nM
DYRK1A
  • IC50:55 nM
Inhibitor
50 nM - 1000 nM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
none identified
Selectivity Assessment Description:
KH-CB19 was profiled against a panel of 71 protein kinases (see Manley et al. [2010] for panel membe ...

Potency
Cellular
In Vitro

CLK1

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1016/j.chembiol.2010.11.009

CLK4

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1016/j.chembiol.2010.11.009

DYRK1A

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1016/j.chembiol.2010.11.009

Chemical Information

Molecular Formula C15H13Cl2N3O2
SMILEs CCOC(=O)c1c(/C(C#N)=C\N)c2ccc(Cl)c(Cl)c2n1C
InChI InChI=1S/C15H13Cl2N3O2/c1-3-22-15(21)14-11(8(6-18)7-19)9-4-5-10(16)12(17)13(9)20(14)2/h4-6H,3,18H2,1-2H3/b8-6-
Molecular weight 337.04 Da
AlogP 3.484980000000001
HBond acceptors 5
HBond donors 2
Atoms 35

References

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Expert Reviews

by SERP
(on 7 Oct 2016 )
Cellular Use Rating
Cellular activity of the compound was confirmed at 1-10 microM by reduced level of phosphorylated SRp55, SRp75 or other SR proteins. KH-CB19 should be used carefully for dissecting splicing machinery...
by SERP
(on 10 Jan 2017 )
Cellular Use Rating
In Model Organisms
I would use KH-CB19 with caution; the profile of this compound needs to be developed further. The compound inhibits multiple CLKs (CLK1&3 - although it is somewhat selective for CLK1 over CLK3 in vitro)....
by SERP
(on 21 Jan 2017 )
Cellular Use Rating
Target-related cellular activity was demonstrated at concentrations of 1-10 uM, which seems high relative to the reported enzymatic activity (IC50 <100 nM). Given that there are no data on the compound's...
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