TAK-981

Inhibitor of SAE1, UBA2

Structure

Information

  • SAE1
  • UBA2
  • Inhibitor
  • Up to 1 uM, followed by washout

In Vitro Validations

Uniprot ID: Q9UBE0
Target Class: Enzyme
Target SubClass: SUMOylation Enzyme
Potency: IC 50
Potency Value: 1 nM
Potency Assay: The E1-E2 HTRF transthiolation (HTRF)
PDB ID for probe-target interaction (3D structure): 6XOH
Structure-activity relationship: yes
Target aliases:
SUMO-activating enzyme subunit 1, UBLE1A, SUA1, AO ...

DOI Reference: 10.1021/acs.jmedchem.0c01491

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:
IC50s of NAE and UAE are 960 and >1000 nM, respectively.
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SERP ratings and comments


SERP Ratings

In Cell Rating
In Model Organisms

(last updated: 13 Sept 2021 )

SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

TAK-981 is a potent and SAE selective modulator of sumoylation occupying ATP binding pocket and forming a SUMO−TAK-981 adduct. The compound is efficacious in cells and animal xenograft models.

(last updated: 6 Oct 2021 )