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CC-90009

CC-90009 : Molecular Glue, degrader of GSPT1

Structure

Information

  • GSPT1
  • Molecular Glue, Degrader
  • 100 nM

In Vitro Validations

Uniprot ID: P15170
Target Class: Other
Target SubClass: Translation Termination Factor
PDB ID for probe-target interaction (3D structure): 6XK9
Structure-activity relationship: yes
Target aliases:
Eukaryotic peptide chain release factor GTP-bindin ...

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

Proteomics: Proteomic experiments with concentration range from 0.20 μM up to 3 μM with 4 or 6 h incubation shows GSPT1 is the only detectable protein degraded with greater than ∼75% degradation.

Ouside Target Family: Selective in its degradation over other proteins (IKZF1/3 EC50 > 10 μM). CC-90009 (up to 3 μM) did not inhibit P-gp, BCRP, MRP2, OAT1, OAT3, OATP1B1, OATP1B3, OCT2, or MATE2-K. CC-90009 was screened against a diverse panel of 255 kinases at 3 μM with no inhibition observed >20%. The selectivity of CC-90009 was explored against 80 different human receptors, ion channels, and transporters, and at a concentration of 10 μM, CC-90009 inhibited receptor binding ≥50% at only two receptors, M1(h) and M2(h). No inhibition or induction of cytochrome P450 (CYP) enzymes in in vitro studies except for weak inhibition of CYP2C9 (41% at 2.5 μM) and CYP2C19 (IC50 = 1.53 μM).

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SERP ratings and comments

SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

CC-90009 is a potent, highly selective and thoroughly characterised molecule for investigating effects of GSPT1 degradation both in cells and a range of in vivo models.

(last updated: 17 Dec 2021 )

SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

CC-90009 is a well-validated drug candidate that can also be used as a chemical probe to degrade GSPT1.

(last updated: 20 Dec 2021 )