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GPX4-IN-5 | GPX4-IN-5 : Covalent Inhibitor of GPX4
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (3 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
GPX4
  • IC50:120 ± 10 nM
  • ΔTm:6.5
  • IC50:10-75 nM
Covalent Inhibitor
up to 1 uM

Selectivity

In Cell Selectivity Assessment
Potency Assay Off-Target:
MDA-MB-231 incubated with compounds alone and with compounds and Fer-1 (Ferropotosis inhibitor, 1 uM ...

Potency
Cellular
In Vitro

GPX4

Mode of Action: Covalent Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.3c00967

In Vivo Validations

Mouse
Dose: 10 mg/Kg
Route of delivery: Intraperitoneal
Plasma half life: 1.90 ± 0.42 h
Systemic clearance: 0.83 ± 0.37 L/h/kg
Cmax: 5205 ± 905 ng/mL
Tmax: 0.85 ± 0.20 h
Area Under the Curve:: 12,099 ± 3689 ng/L·h

DOI Reference: 10.1021/acs.jmedchem.3c00967

Negative Control Compounds

ferrostatin-1
Notes: Fer-1 can be used in combination with GPX4-Inhibitor-C18 as negative control at concentration 1 uM

Chemical Information

Molecular Formula C18H17ClFNO5
SMILEs COc1cc(N(C(=O)CCl)c2ccc3c(c2)OCCO3)cc(OC)c1F
InChI InChI=1S/C18H17ClFNO5/c1-23-15-8-12(9-16(24-2)18(15)20)21(17(22)10-19)11-3-4-13-14(7-11)26-6-5-25-13/h3-4,7-9H,5-6,10H2,1-2H3
Molecular weight 381.08 Da
AlogP 0.0
HBond acceptors 6
HBond donors --
Atoms 43

References

Publications

Cross References

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Vendors

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Expert Reviews

by SERP
(on 11 Oct 2023 )
Cellular Use Rating
In Model Organisms
I am somewhat unconvinced by the presented data on this compound as being wholly on-target and therefore useful as a chemical probe. Specifically: - biochemical inhibition data are expressed as %age inhibition...
by SERP
(on 22 Oct 2023 )
Cellular Use Rating
In Model Organisms
C18 demonstrates biologically potent on-target inhibition of GPX4 leading to ferroptosis induction of susceptible cell lines. It is active in vivo in tumour models susceptible to ferroptosis mediated cell...
by SERP
(on 3 Nov 2023 )
Cellular Use Rating
In Model Organisms
in vivo dose-response not seen above 10 mg/Kg
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