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Capzimin | Capzimin : Inhibitor of Rpn11
RATINGS:
Cellular Use: (1 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
PSMD14
  • IC50:360 nM
  • IC50:600 nM
  • GI50:~2000 nM
Inhibitor
up to 10 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
Capzimin showed 80-fold selectivity for Rpn11 over Csn5, ten-fold over AMSH and six-fold over BRCC36 ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
Capzimin was screened against the NCI panel of 60 cancer cell lines31. The median GI50 was 3.3 μM (S ...

Potency
Cellular
In Vitro

PSMD14

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.6b01379

Chemical Information

Molecular Formula C30H24N6O2S4
SMILEs O=C(NCCc1nccs1)c1cnc2c(SSc3cccc4cc(C(=O)NCCc5nccs5)cnc34)cccc2c1
InChI InChI=1S/C30H24N6O2S4/c37-29(33-9-7-25-31-11-13-39-25)21-15-19-3-1-5-23(27(19)35-17-21)41-42-24-6-2-4-20-16-22(18-36-28(20)24)30(38)34-10-8-26-32-12-14-40-26/h1-6,11-18H,7-10H2,(H,33,37)(H,34,38)
Molecular weight 628.08 Da
AlogP 6.4404
HBond acceptors 8
HBond donors 2
Atoms 66

References

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canSARChEMBLBindingDB

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Expert Reviews

by SERP
(on 7 Nov 2023 )
Cellular Use Rating
The compound elicits a phenotype that is consistent with inhibition of proteasomal deubiquitination by PSMD14 and is distinct from proteasome inhibitors targeting the catalytic subunits. However, researchers...
Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria