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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
Vendors
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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 0.0
HBond acceptors 8
HBond donors 4
Atoms 44

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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