ABD957

Covalent Inhibitor of ABHD17B

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(0 ratings)

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Probe ABD957 is in the process of SERP review.

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Information

ABHD17B

Covalent Inhibitor

up to 1 uM

Probe Availability:

MedChemExpress

In Vitro Validations

Uniprot ID: Q5VST6

Target Class: Other post-translational modification

Target SubClass: Depalmitoylase

Potency: IC50

Potency Value: 210 nM ABHD17B

Potency Assay: Gel-based activity-based protein profiling assay

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

Target aliases:

Alpha/beta hydrolase domain-containing protein 17B ...

DOI Reference: 10.1038/s41589-021-00785-8

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

LYPLA1 IC50 10 uM in cell lysate

Probe Selectivity in Cell:

MS-ABPP data for ABD957 (500 nM, 2 h) in OCI-AML3 cells confirmed ABHD17A/B/C inhibition and selectivity across the majority of quantified serine hydrolases, including LYPLA1, LYPLA2 and ABHD10

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SERP ratings and comments

SERP Ratings

In Cell Rating

SERP Comments:

ABD957 is a covalent inhibitor of several serine hydrolases. Activity-based proteomics confirmed inhibition of ABHD17A/B/C and other targets including CES2, ABHD6, CES1 and ABHD13. Please note that due to covalent binding of the inhibitors all effects are time-dependent and selectivity is a snapshot at a particular point in time. Compared to ABD957 other reported ABHD17 inhibitors such as Palm B, Palm M and HDFP show a lower selectivity and are also covalent inhibitors. In vitro studies demonstrated that ABD957 was able to attenuate ABHD17-mediated N-Ras depalmitoylation in AML cells.

(last updated: 8 Apr 2025 )