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OICR-8268

OICR-8268 : Inhibitor of DCAF1

Structure

Information

  • DCAF1
  • Inhibitor
  • up to 20 uM
  • Reviewer recommended concentration: 10-40 µM as no maximal effect seen with 10 µM in CETSA

In Vitro Validations

Uniprot ID: Q9Y4B6
Target Class: Structural protein
Target SubClass: --
Potency: Kd
Potency Value: 38 nM
Potency Assay: SPR
PDB ID for probe-target interaction (3D structure): 8F8E
Target aliases:
DDB1- and CUL4-associated factor 1, VPRBP, RIP, KI ...

DOI Reference: 10.1021/acs.jmedchem.2c02132

Uniprot ID: Q9Y4B6
Target Class: Structural protein
Target SubClass: --
Potency: Kd
Potency Value: 216 ± 76 nM
Potency Assay: ITC
PDB ID for probe-target interaction (3D structure): 6S4F
Target aliases:
DDB1- and CUL4-associated factor 1, VPRBP, RIP, KI ...

DOI Reference: 10.1021/acs.jmedchem.2c02132

In Cell Validations

In Vivo Data

No in Vivo Validations

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SERP ratings and comments

SERP Ratings

In Cell Rating

SERP Comments:

OICR-8268 is a highly potent DCAF1 ligand and a very useful tool compound to interrogate this E3 ligase substrate adaptor. The binding mode of the compound is backed up by a co-crystal structure and extensive SAR data, the potency was determined by orthogonal biophysical interaction assays and cellular target engagement is demonstrated through CETSA. However, specificity analysis for other DCAF proteins, effectivity in other cell lines and toxicity data would be welcome additions in the future. Researchers using this compound are advised to include a phenotyptic assay for DCAF1 inhibition/engagement in their experiments, as cellular use of the compound has currently been restricted to the CETSA assay (up to the time of this review in March 2024).

(last updated: 20 Mar 2024 )

SERP Ratings

In Cell Rating

(last updated: 22 Mar 2024 )