BI-1935

Inhibitor of EPHX2

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(1 ratings)

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Probe BI-1935 is in the process of SERP review.

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Information

EPHX2

Inhibitor

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Additional Data

SGC image SGC Chemical Probe Collection

Probe Availability:

MedChemExpress

In Vitro Validations

Uniprot ID: P34913

Target Class: Other

Target SubClass: Epoxide Hydrolase 2

Potency: IC50

Potency Value: 7 nM

Potency Assay: biochemical h-sEH binding assay

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

Structure-activity relationship: yes

Target aliases:

Bifunctional epoxide hydrolase 2, EPHX2, HYES_HUMA ...

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Internal screen against hCYP epoxygenases 2J2/2C9/2C19 and IL-2: > 100-fold selectivity achieved (> 1μM for all)

Probe Selectivity in Cell:

Off Target Screen - Panlabs panel: 61/67 < 20% Inhibition @ 10 μM, 5/67 < 80% Inhibition @ 10 μM, Thromboxane Synthase 96% inhibition @ 10 μM (IC50 = 0.132 μM)

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

BI-1935 is a potent and selective small-molecule inhibitor of soluble epoxide hydrolase (sEH). Its activity is demonstrated by both in vitro (biochemical binding assay h-sEH = IC50 of 7 nM) and cellular analysis (cellular Hep G2-DHET assay format = IC50 of < 1 nM). It also has a good selectivity against hCYP epoxygenases 2J2/2C9/2C19 and IL-2. An Eurofins-Panlabs panel was measured against 67 targets (data available).

This molecule can be used in vivo: it showed a dose dependent effect on mean arterial pressure blood pressure in Dahl salt sensitive rats (spontaneous hypertensive rats (SHR) can also be employed in in vivo studies).

Furthermore, the compound BI-2049 (free access) can be used as in vitro negative control (IC50 h-sEH = >100 µM).

No X-ray co-crystal structure of the probe and the target protein is available to date (July 2020).

The compound is recommended for both in vitro and in vivo research to investigate the biology of sEH

(last updated: 3 Jul 2020 )