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. 2023 Jul 18;14:4297. doi: 10.1038/s41467-023-40086-3

Fig. 7. Development of selective HCK inhibitors and identification of BT424 as a specific HCK inhibitor.

Fig. 7

A SAR study of dasatinib to design selective HCK inhibitors. B Screen HCK specific inhibitors for all our designed compounds. Five inhibitors (BT294, 331, 332, 342 and 424) with high efficiency of HCK inhibitions are highlighted in red arrows. C HCK inhibition profiling for BT424 with 10 dose 1:3 serial dilution. D Inhibition of all SFKs for 6 candidate HCK inhibitors at 50uM. SFKs inhabitation assay was performed at Reaction Biology Corp. Values were shown for % of enzyme activity compared to DMSO control. Cell proliferation (E) and cytotoxicity (F) were measured by MTT assay and release LDH with various concentration of BT424 for 24 h in Raw264.7 cells. Source data are provided as a Source Data file.