BI-99179

BI 99179 : Inhibitor of FASN

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(2 ratings)

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Probe BI-99179 is in the process of SERP review.

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Information

FASN

Inhibitor

1-10 uM

Additional Data

SGC image SGC Chemical Probe Collection

Probe Availability:

In Vitro Validations

Uniprot ID: P49327

Target Class: Enzyme

Target SubClass: Synthase

Potency: IC50

Potency Value: 79 nM

Potency Assay: Inhibition of FASN

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

Target aliases:

, Fatty acid synthase, FAS, FASN, FAS_HUMAN, Type ...

DOI Reference: 10.1016/j.bmcl.2011.07.083

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

Selectivity within target family: No closely related mammalian proteins as potential off-targets. Selectivity outside target family: External screen covering 30 non-related targets: <20% inhibition @ 10 µM for all targets The only hit in the GPCR scan is DAT/SLC6A3 (77.27 % inhibition). A few kinases from the panel showed <50% of the control in the kinome scan when tested @ 1 uM.

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

(last updated: 9 Feb 2022 )

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

The compound was independently tested in an NADPH consumption assay (Singha et. al. Eur. Journal Pharm. Sciences 2020, 149, 105321) alongside GSK2194069, another FAS inhibitor reported in 2014 and was found to indeed be active (IC50 = 13 nM) and ca. 3x more potent than GSK2194069 (IC50 = 41 nM)

(last updated: 18 Feb 2022 )