Relacatib

Inhibitor of CTSK, CTSL, CTSV

Structure

Information

  • CTSK
  • CTSL
  • CTSV
  • Inhibitor
  • up to 500 nM
  • Reviewer recommended concentration: up to 1 uM

In Vitro Validations

Uniprot ID: P43235
Target Class: Protein metabolism
Target SubClass: Protease
Potency: Ki
Potency Value: 0.041 nM
Potency Assay: Cathepsin K Proteolytic Catalytic Activity assay
PDB ID for probe-target interaction (3D structure): 2FTD
Structure-activity relationship: yes
Target aliases:
Cathepsin K, CTSO2, CTSO, CTSK, CATK_HUMAN, Cathep ...

DOI Reference: 10.1021/jm050915u

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency end-point : Ki CTSS 1.6 nM, CTSB 13 nM
Probe Selectivity in Vitro:
Exhibits 39–300-fold selectivity over other cathepsins.
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SERP ratings and comments


SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

This is an excellent probe. Rated 3* (rather than 4*) because it acts on more than one target.

(last updated: 16 Nov 2020 )

SERP Ratings

In Cell Rating
In Model Organisms

(last updated: 3 Dec 2020 )

SERP Ratings

In Cell Rating
In Model Organisms

(last updated: 14 Dec 2020 )