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MR24 | MR24 : Inhibitor of STK24, STK26
RATINGS:
Cellular Use: (3 reviews)

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

Targets Biochemical/Biophysical Potency Cellular Potency
STK24
  • ΔTm:10.6 ± 0.1 °C
  • EC50:81 nM
  • EC50:57 ± 44 nM
STK26
  • ΔTm:8.1 ± 0.1 °C
  • EC50:583 ± 210 nM
Inhibitor
up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
Selective in a panel of 100 kinases: in the DSF panel assay against 100 kinases, MR24 (24) stabilize ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
MR24 showed no cellular binding for MST1/2 in NanoBRET assays (EC50 values >50 μM). MR24 only weakly ...

Potency
Cellular
In Vitro

STK24

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.3c02217

STK26

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.3c02217

Orthogonal Probes def

3FE

Chemical Information

Molecular Formula C26H29ClN6O3
SMILEs Cc1cccc(-c2ccc(-c3cc4cnc(NC(CO)CO)nc4n(CCCCN)c3=O)c(Cl)c2)n1
InChI InChI=1S/C26H29ClN6O3/c1-16-5-4-6-23(30-16)17-7-8-20(22(27)12-17)21-11-18-13-29-26(31-19(14-34)15-35)32-24(18)33(25(21)36)10-3-2-9-28/h4-8,11-13,19,34-35H,2-3,9-10,14-15,28H2,1H3,(H,29,31,32)
Molecular weight 508.20 Da
AlogP 0.0
HBond acceptors 9
HBond donors 5
Atoms 65

References

Publications

Cross References

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Expert Reviews

by SERP
(on 4 Apr 2024 )
Cellular Use Rating
MR24 is an inhibitor of MST3 and MST4. The approach to measuring selectivity was by screening a representative panel of kinases using DSF (thermal shift) in vitro and then testing kinases with an observed...
by SERP
(on 25 Apr 2024 )
Cellular Use Rating
STK24 pharmacology may dominate at concentrations in the 10 nM - 100 nM range.
by SERP+
(on 23 May 2024 )
Cellular Use Rating
Cell potency was at the maximum limit of 1 micromolar.
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