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IBERDOMIDE

IBERDOMIDE : Modulator of CRBN, Molecular glue IKZF1, IKZF3

Structure

Information

  • CRBN
  • IKZF1
  • IKZF3
  • Modulator
  • Molecular Glues
  • 10-100 nM

In Vitro Validations

Uniprot ID: Q96SW2
Target Class: Post-translational
Target SubClass: E3 Ligase
Potency: IC50
Potency Value: 60 nM
Potency Assay: TR-FRET cereblon binding assay
PDB ID for probe-target interaction (3D structure): 7PS9,  5V3O
Target aliases:
Protein cereblon, CRBN, CRBN_HUMAN

DOI Reference: 10.1021/acs.jmedchem.6b01921

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Potency assay, off target (cells): Treatment of B cells with Iberdomide (10 nM for 24 hours) resulted in a significant decrease in the protein levels of Ikaros (66 kDa isoform) and Aiolos (58 kDa isoform), but not the other Ikaros family zinc finger factors Helios (IKZF2) or Pegasus (IKZF5). Expression of Eos (IKZF4) was not detected in B cells. Treatment of T cells with Iberdomide (10 nM for 24 hours) resulted in a significant decrease in the protein levels of Ikaros (58 and 66 kDa isoforms) and Aiolos (58 and 80 kDa isoforms), but not Helios, Eos or Pegasus. Another zinc finger protein with sequence homology to Ikaros and Aiolos, Zinc Finger Protein 91 (ZFP91), was significantly reduced by Iberdomide (10 nM for 24 hours) in B cells. no significant degradation of GSPT1 or CK1alpha.
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SERP ratings and comments

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