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HRX215 | HRX215 : Inhibitor of MAP2K4
RATINGS:
Cellular Use: (1 reviews)

In Model Organisms: (1 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
  • IC50:20 nM
  • % in:>70%
Inhibitor
up to 3 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
>100-fold selectivity against JNK1, BRAF, and MKK7
In Cell Selectivity Assessment
Potency Assay Off-Target:
MRNA sequencing and transcriptomic analyses
Selectivity Assessment Description:
analysis was conducted with mRNA obtained from hepatectomized mouse livers with shRNA-mediated MKK4 ...

Potency
Cellular
In Vitro

MAP2K4

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1016/j.cell.2024.02.023

In Vivo Validations

Mouse
Dose: 30 mg/Kg
Route of delivery: Oral
Plasma half life: 3.4 h
Cmax: 53.51 uM
Area Under the Curve:: 66.62 uM*h

DOI Reference: 10.1016/j.cell.2024.02.023

Chemical Information

Molecular Formula C21H19F2N5O3S
SMILEs CCCS(=O)(=O)Nc1c(F)cc(C(=O)C2=NNC3NC=C(c4ccncc4)C=C23)cc1F
InChI InChI=1S/C21H19F2N5O3S/c1-2-7-32(30,31)28-19-16(22)9-13(10-17(19)23)20(29)18-15-8-14(11-25-21(15)27-26-18)12-3-5-24-6-4-12/h3-6,8-11,21,25,27-28H,2,7H2,1H3
Molecular weight 459.12 Da
AlogP 2.550200000000001
HBond acceptors 8
HBond donors 3
Atoms 51

References

Publications

Cross References

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Expert Reviews

by SERP
(on 13 Aug 2024 )
Cellular Use Rating
In Model Organisms
Structure-guided optimization of the MKK4 off-target activity of vemurafenib culminated in the identification of HR215 which is currently investigated in clinical trials for the treatment of liver failure....
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