ATABECESTAT

ATABECESTAT : Inhibitor of BACE1, BACE2

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(2 ratings)

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Probe ATABECESTAT is in the process of SERP review.

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Information

BACE1
BACE2

Inhibitor

100 nM (inhibition of both BACE1 and BACE2)

Probe Availability:

In Vitro Validations

Uniprot ID: P56817

Target Class: Enzyme

Target SubClass: Protease

Potency: IC50

Potency Value: 9.8 nM

Potency Assay: Biochemical homogeneous time-resolved fluorescence (HTRF)-based assay

PDB ID for probe-target interaction (3D structure): 7DCZ

Target aliases:

Beta-secretase 1, KIAA1149, BACE, BACE1, BACE1_HUM ...

DOI Reference: 10.1021/acs.jmedchem.0c01917

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

Inhibited BACE2 (IC50 = 5.6 nM) with comparable potency as for BACE1, whereas it was extremely selective over CatD and CatE (IC50 = >100 μM).

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

Overall a good probe in terms of potency and PK profile. However, the lack of selectivity over BACE2 may lead to incorrect conclusions in phenotypic screens. It is recommended to use this probe with a selective BACE2 inhibitor (as orthogonal probe) to aid target deconvolution (e.g. https://doi.org/10.1002/cmdc.201800725)

(last updated: 14 Apr 2022 )

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

This is a useful probe for BACE1 and BACE2 inhibition. Data obtained from the employment of this probe should be interpreted as inhibition of both targets, not just one.

(last updated: 1 May 2022 )