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JA310 | JA310 : Inhibitor of STK24
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:7.5 ± 0.6 Kelvin
  • IC50:76 nM
  • EC50:106 nM
Inhibitor
up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
DSF confirmed stabilization of MST3 and MST4 but not MST2 and MST3. Outside the MST family, JA310 st ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
In NanoBRET, JA310 showed comparatively weaker activity for MST4, with EC50 values of 1.4 μM and 362 ...

Potency
Cellular
In Vitro

STK24

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.3c01980

Negative Control Compounds

JA262
Notes: Control was inactive in NanoBRET
SMILES: O=C(NCCOCCNC1=NC2=C(Cl)C=N1)C3=CC(N2)=NN3

Chemical Information

Molecular Formula C17H19N7O
SMILEs O=C1NCCCCCNc2nc(c3ccccc3n2)Nc2cc1[nH]n2
InChI InChI=1S/C17H19N7O/c25-16-13-10-14(24-23-13)21-15-11-6-2-3-7-12(11)20-17(22-15)19-9-5-1-4-8-18-16/h2-3,6-7,10H,1,4-5,8-9H2,(H,18,25)(H3,19,20,21,22,23,24)
Molecular weight 337.17 Da
AlogP 2.4220999999999995
HBond acceptors 8
HBond donors 4
Atoms 44

References

Publications

Cross References

ChEMBL BindingDB PDB PubChem canSAR SGC

Expert Reviews

by SERP
(on 24 Mar 2024)
Cellular Use Rating
Macrocyclic compound JA310 demonstrates exquisite selectivity across the kinome. Selectivity against closely related isoform MST4 is 4-5fold in permeabilized cells. What is not immediately clear, is the...
by SERP+
(on 23 May 2024)
Cellular Use Rating
The chemical probe achieved remarkable selectivity whithin the kinome (340 wild-type kinases) due to its macrocyclic nature. Moreover, it is an ATP-competitive inhibitor that also induces conformational...
by SERP+
(on 17 Jun 2024)
Cellular Use Rating
This is a highly potent probe with high selectivity over 340 kinases. No toxicity at concentrations lower than 2 µM has been observed. The compounds seemd to possess sufficient solubility for typical...
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