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MU1210 | MU1210 : Inhibitor of CLK1, CLK2, CLK4
RATINGS:
Cellular Use: (3 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
CLK1
  • IC50:8 nM
  • Ki:84 nM
CLK2
  • IC50:20 nM
  • Ki:91 nM
CLK4
  • IC50:12 nM
  • Ki:23 nM
Inhibitor
500 nM
up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
MU1210 is selective in a panel of 210 kinases in an activity-based assay (Invitrogen) at 1 µM. The c ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
HIPK2 and GSK3A/B activity was analysed via NanoBRET in cells and reported not active at 10uM agains ...

Potency
Cellular
In Vitro

CLK1

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1016/j.ejmech.2021.113299

CLK2

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1016/j.ejmech.2021.113299

CLK4

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1016/j.ejmech.2021.113299

Negative Control Compounds

MU140
Notes: not active in NanoBRET up to 3 uM.

Orthogonal Probes def

T3-CLK
SGC-CLK-1

Chemical Information

Molecular Formula C22H16N4O
SMILEs Cn1cc(-c2ccc3occ(-c4cccc(-c5ccncc5)c4)c3n2)cn1
InChI InChI=1S/C22H16N4O/c1-26-13-18(12-24-26)20-5-6-21-22(25-20)19(14-27-21)17-4-2-3-16(11-17)15-7-9-23-10-8-15/h2-14H,1H3
Molecular weight 352.13 Da
AlogP 0.0
HBond acceptors 5
HBond donors --
Atoms 43

Expert Reviews

by SERP
(on 19 May 2023 )
Cellular Use Rating
( The reviewer did not leave any comments )
by SERP+
(on 17 Jun 2024 )
Cellular Use Rating
Chemical probe for CLK1, CLK2, CLK4 with nanomolar potency in biochemical (radiometric assay) and cell-based (NanoBRET) assays. Kinase selectivity was tested in a panel of 210 kinases. HIPK2 (activity-based...
by SERP+
(on 23 Sept 2024 )
Cellular Use Rating
This compound shows good in vitro potency of 8/20/12 nM for CLK1/2/4, respectively. Also it has good cellular potency of 84/91/23 nM for CLK1/2/4, respectively. It was screened for 210 kinases in an activity-based...
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