ERK5-IN-4 (compound 34b) is a potent and selective inhibitor ofextracellular signal-related kinase 5(ERK5). ERK5-IN-4 inhibitsERK5(full-length) and truncatedERK5(ERK5 ΔTAD) kinase activity in HEK293 cells with anIC₅₀of 77 nM and 300 nM, respectively^[1].

ERK5-IN-4 (compound 34b) is selective against MAP3K, p38 (IC₅₀>30 μM) and BRD4 (IC₅₀>20 μM), in contrast to many reported ERK5 inhibitors^[1].
ERK5-IN-4 (0-100 μM; 72 h) suppresses ERK5 kinase activity in HEK293 cells and (0-1 μM; 72 h) induces paradoxical activation of ERK5 transcriptional activity, thus resulting in C-terminal transcriptional activation domain (TAD) separated from the nuclear localization sequence (NLS) and results ERK5 nuclear translocation^[1].
ERK5-IN-4 inhibits cancer cells with GI₅₀of 19.6 μM (HEK293), 22.3 μM (A498), 25 μM (SJSA-1), 26.6 μM (MDA-MB-231) following a 72 h incubation^[1].
ERK5-IN-4 exhibits kinome selectivity K_dof 1.2 μM, 0.29 μM, 0.046 μM, 0.061 μM, 0.18 μM, 0.38 μM, 1.3 μM, 0.42 μM, 0.22 μM, 2.8 μM against ABL1-nonphosphorylated, AURKA, CSF1R, DCAMKL1 (DCLK1), ERK5 (MAPK7), FGFR1, JAK3 (JH1domain-catalytic), KIT, LRRK2, MEK5 (MAP2K5)^[1].

ERK5-IN-4 (compound 34b) (p.o.; 10 mg/kg) has low clearance and an oral bioavailability of 42% in the mouse^[1].

381.19

C₁₆H₁₁Cl₂FN₄O₂

1888305-17-6

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