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BSJ-04-122 | BSJ-04-122 : Covalent of MAP2K4, MAP2K7
RATINGS:
Cellular Use: (2 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
MAP2K4
  • IC50:4 nM
  • % in:87.0%
  • % in:~100%
MAP2K7
  • IC50:181 nM
  • IC50:707 nM
  • % in:90.2%
Covalent
up to 10 uM

Selectivity

In Cell Selectivity Assessment
Potency Assay Off-Target:
MKK4 and MKK7 are the top targets bound by BSJ-04-122 in MDA-MB-231 cells pretreated with the compou ...
In Vitro Selectivity Assessment
Potency Assay Off-Target:
BSJ-04-122 was profiled against a broader kinase panel using the KINOMEscan approach: a total of 26 ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
Selectivity within target family: BSJ-04-122 had no effect on the phosphorylation of p38, a downstr ...

Potency
Cellular
In Vitro

MAP2K4

Mode of Action: Covalent

Structure-Activity-Relationship data available? No

DOI Reference: 10.1016/j.chembiol.2020.08.014

MAP2K7

Mode of Action: Covalent

Structure-Activity-Relationship data available? No

DOI Reference: 10.1016/j.chembiol.2020.08.014

Negative Control Compounds

N-(2-((5-chloro-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)phenyl)propionamide
Notes: BSJ-04-122-R (cpd 3R) IC50 6510 nM MKK4

Chemical Information

Molecular Formula C15H12ClN5O
SMILEs C=C/C(O)=N/c1ccccc1Nc1ncnc2[nH]cc(Cl)c12
InChI InChI=1S/C15H12ClN5O/c1-2-12(22)20-10-5-3-4-6-11(10)21-15-13-9(16)7-17-14(13)18-8-19-15/h2-8H,1H2,(H,20,22)(H2,17,18,19,21)
Molecular weight 313.07 Da
AlogP 0.0
HBond acceptors 6
HBond donors 3
Atoms 34

References

Publications

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Expert Reviews

by SERP
(on 4 Jan 2023 )
Cellular Use Rating
There may be cross-reactivity with other kinases at 10uM, as quite a few kinases are nearly completely inhibited by this compound at 1uM (in biochemical assays). Thus, it would be wise to perform experiments...
by SERP+
(on 22 Mar 2023 )
Cellular Use Rating
( The reviewer did not leave any comments )
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