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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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