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BAY-091

2D structure
Target PIP4K2A 
Targeted domain Kinase domain (active site)
Mode of action Inhibitor (type 1, ATP competitive)
Control BAY-0361
Recommended cellular usage concentration 1 - 10 µM
In vivo use No
Synonyms Compound 60
Donated by Bayer


Probe criteria


Inhibitor/agonist potency: goal is < 100 nM (IC50, Kd) Surpasses criterion: Quantification of produced ADP: IC50 = 1.3 nM (10 µM ATP), 2.6 nM (250 µM ATP)
Quantification of produced PI(4,5)P2 (Homogeneous Time Resolved Fluorescence (HTRF):): IC50 = 8.5 nM (10 µM ATP), 16.4 nM (2 mM ATP)
Eurofins kinase panel (at 1 µM): IC50 = 21 nM
Selectivity within target family: > 30-fold Eurofins Kinase Panel (373 kinases at 1 µM): No off-target kinase inhibition > 60 %
In the CETSA assay (intact K-562 cells, 1 h , 37°C) a shift was observed for PIP4K2B at 3 µM.
Selectivity outside target family Eurofins safety panel (77 targets at 10 µM): Closest off-targets [% inhibition]: TBXAS1 (98 %), HTR2B (98 %), MAOB (81 %), PDE3 (74 %), PDE5A (62 %)
PDSP scan (44 targets) at 10 µM clean except for HTR2B (Ki = 1502.8 nM) and GABAA/BZP (Ki = 6834.39 nM)
On target cell activity for cell-based targets: goal is < 1 µM IC50/EC50 Surpasses criterion: Cellular PIP4K2A target engagement proven: CETSA lysates, 60°C: EC50 (95% CI) = 1.8 µM (1.4 -2.2 µM); CETSA int. cells, 56°C: EC50 (95% CI) = 1.1 µM (0.9 – 1.4 µM)
No effect in cellular mechanistic (pAKT, ROS) or functional assays (p53 mutant proliferation).
Control compound (100 times less potent than the probe) BAY-0361: Eurofins kinase panel at 1 µM: IC50 = 271 nM (~ 18-fold)
No shift was observed in the CETSA assay (intact K-562 cells, 1 h , 37°C) for PIP4K2A and PIP4K2B at 30 µM.
Clean PDSP scan (44 targets) at 10 µM