BAY-297 

BAY-297 is a PIP4K2A inhibitor. BAY-297 binds to PIP4K2A in intact cells and cell lysates. BAY-297 serves as a chemical probe for investigating the PIP4K2A signaling pathway and its roles in physiological conditions such as cancer^[1].

BAY-297 (¹³-69 nM; 60 min) potently inhibits recombinant PIP4K2A kinase activity with IC₅₀ values of 13 nM (10 μM ATP) and 69 nM (250 μM ATP) in an ATP consumption assay^[1].
BAY-297 (110-769 nM; 20 min) inhibits recombinant PIP4K2A kinase activity with IC₅₀ values of 110 nM (10 μM ATP) and 769 nM (2 mM ATP) in an HTRF binding competition assay^[1].
BAY-297 (2.1 μM; 30 min) engages with PIP4K2A in THP-1 cell lysates, as measured by a CETSA with an EC₅₀ of 2.1 μM^[1].
BAY-297 (2.3->10 μM) inhibits CYP2C8 (IC₅₀ 2.3 μM), CYP2C9 (IC₅₀ 3.4 μM), and CYP3A4 (IC₅₀ 10 μM, time-dependent IC₅₀ 8.35 μM) in human liver microsomes, with no significant inhibition of CYP1A2 or CYP2D6^[1].
BAY-297 (3.1 μM) inhibits hERG K⁺ currents in recombinant HEK293 cells with an IC₅₀ of 3.1 μM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

459.90

C₂₅H₁₉ClFN₅O

3032120-57-0

CC[C@@H](NC1=C(C#N)C(C2=CC=C(C3=C(F)C(Cl)=CC=C3)C=C2)=NC4=CN=CC=C41)C(N)=O

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• [1]. Wortmann L, et al. Discovery and Characterization of the Potent and Highly Selective 1,7-Naphthyridine-Based Inhibitors BAY-091 and BAY-297 of the Kinase PIP4K2A. J Med Chem. 2021 Nov 11;64(21):15883-15911.  [Content Brief]