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BI 99179

2D structure
Target FASN 
Targeted domain Ketoacyl Reductase domain
Mode of action Inhibitor
Control BI 99990
Recommended cellular usage concentration 1 -10 µM
In vivo use No
Donated by Boehringer Ingelheim


Probe criteria


Inhibitor/agonist potency: goal is < 100 nM (IC50, KD) Inhibition of FASN: IC50 = 0.079 µM
Selectivity within target family: > 30-fold 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 PDSP scan is SLC6A3 (77.27 % inhibition).
On target cell activity for cell-based targets: goal is < 1 µM IC50/EC50 1. Inhibition of [14C]acetate incorporation into mouse N-42 cells: IC50 = 0.57 µM
2. Inhibition of [14C]acetate incorporation into human H1975 cells: IC50 = 0.18 µM
Control compound (100 times less potent than the probe) Inhibition of FASN: >3 µM for inactive analog BI 99990; Shows weak off-target activity in the PDSP scan for TMEM97 (Sigma2) (Ki = 396.0 nM) and HRH4 (Ki = 1635.0 nM).