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. 2017 Mar 8;7:43908. doi: 10.1038/srep43908

Figure 2. Lead compounds RU-301 and RU-302 show inhibitory activity in blocking TAM signaling.

Figure 2

(A) Schematic representation of wild-type and chimeric TAM receptors. (B) Activation of the TAM-IFNγR1 chimeric receptors with Gas6 with pSTAT1 phosphorylation as readout for TAM activation. (C) Summary of small molecule inhibitors (10 μM) screening using TAM-IFNγR1 chimeric assay system showing RU-301 and RU-302 as the lead compounds. (D) Dose-response inhibition of Gas6-induced receptor activation by RU-301 (0.625–5.0 μM) using Axl-IFNγR1 cell lines. (E) Dose-response inhibition of Gas6-induced receptor activation by RU-302 (0.625–5.0 μM) using Axl-IFNγR1 cell lines. (F) Comparative inhibition of Gas6-induced receptor activation by 10.0 μM RU-301 and RU-302 on TAMs using TAM-IFNγR1 cell lines. (G,H) Comparison of R428 (a known Axl kinase domain targeting inhibitor) and RU-301 (Axl/Gas6 interaction inhibitor) by KinomeScan™ profiling for kinase domain interactions in the human kinome. Red circles represent drug binding kinases and the diameter of the circles represent the relative binding affinities.