MSC778

MSC778 : Inhibitor of FEN1

Structure

Information

  • FEN1
  • Inhibitor
  • up to 1 uM

In Vitro Validations

Uniprot ID: P39748
Target Class: Enzyme
Target SubClass: Endonuclease
Potency: IC50
Potency Value: 3.0 nM
Potency Assay: Fluorescently labeled 5′-flap cleavage assay
PDB ID for probe-target interaction (3D structure): --
Target aliases:
Flap endonuclease 1, RAD2, FEN1, FEN1_HUMAN, hFEN- ...

DOI Reference: 10.1021/acs.jmedchem.5c01526

Uniprot ID: P39748
Target Class: Enzyme
Target SubClass: Endonuclease
Potency: Kd
Potency Value: 2.9 nM
Potency Assay: SPR
PDB ID for probe-target interaction (3D structure): --
Target aliases:
Flap endonuclease 1, RAD2, FEN1, FEN1_HUMAN, hFEN- ...

DOI Reference: 10.1021/acs.jmedchem.5c01526

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:
Selectivity against other nucleases: EXO1 145-fold GEN1 516-fold XPG 65-folda
Probe Selectivity in Vitro:
MSC778 displayed excellent selectivity against all members of an in-house panel of the broader nuclease superfamily, with MRE11 being the next closest in activity (>1000-fold selectivity).
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