FAH65E(-)

FAH65E(-) : Inhibitor of BACE1

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(2 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.

Probe FAH65E(-) is in the process of SERP review.

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Information

BACE1

Inhibitor

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

In Vitro Validations

Uniprot ID: P56817

Target Class: Enzyme

Target SubClass: Peptidase

Potency: IC50

Potency Value: 5 nM

Potency Assay: P5-P5′ assay

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

Target aliases:

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

DOI Reference: 10.1016/j.neurot.2025.e00610

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): FAH65 was found to be selective for BACE1 as the target enzyme. FAH65 did not significantly inhibited cathepsin D (Cat D) activity, and BACE2 activity compared to BACE-IV. The FAH65 IC50 for Cat D, BACE2, and BACE1 are ∼47 μM, >1 μM and ∼0.01 μM, respectively.

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

The compound should be best used up to 100 nM as at 1 µM some inhibition of BACE2 could be expected. It is also worth noting that the compound has only been tested in B254 mice overexpressing APP.

(last updated: 31 Aug 2025 )

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

To qualify as a probe with four stars the selectivity of FAH65E(-) needs to be shown versus a broader scope of biological targets.

(last updated: 16 Sept 2025 )