Relacatib

Inhibitor of CTSK, CTSL, CTSV

Structure

SERP Rating

In Cells

(3 ratings)

In Model Organisms

(3 ratings)

note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars.

Information

CTSK
CTSL
CTSV

Inhibitor

~~up to 500 nM~~
Reviewer recommended concentration: up to 1 uM

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Probe Availability:

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 )