NVP-BHG712

Unsuitables - unsuitable to be used as a chemical probe

Structure

This is unsuitable as a chemical probe: While this compound has been used to interrogate specific protein targets, it is not a chemical probe and should not be used in assays that depend on a potent and selective modulator of the protein.

Regioisomer-dependent activity

NVP-BHG712 is considered unsuitable as a reliable chemical probe because its reported identity and biological activity are affected by the presence of a regioisomer. Tröster et al. demonstrated that all commercially available samples tested as “NVP-BHG712” were actually the NVP-BHG712 regioisomer (NVPiso), differing only in the position of a single methyl group. Importantly, the two regioisomers exhibit different binding modes, kinase affinities, and selectivity profiles. Consequently, biological results obtained using commercially available NVP-BHG712 may not reflect the activity of the originally described compound. The study therefore highlights significant concerns regarding the reproducibility and interpretation of experiments using NVP-BHG712 as an EPHA2/EPHB4 inhibitor. (⁠DOI:10.1002/cmdc.201800398)

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