MAPK - ERK5

XMD8-92 is a potent and selective BMK1/ERK5 inhibitor .

BAY885 is a novel ERK5 inhibitor.

XMD17-109 is a novel, specific inhibitor of ERK-5 with an EC50 value of 4.2 uM in HEK293 cells.

ERK5-IN-1 exhibits potent inhibition of ERK5 with cellular EC50 values of 0.19 uM and enzymatic IC50 values of 0.087 uM and of LRRK2[G2019S] with enzymatic IC50 values of 0.026uM.

ERK5-IN-2 is an orally active, sub-micromolar, selective ERK5 inhibitor with IC50s of 0.82 μM, 3 μM for ERK5 and ERK5 MEF2D, respectively.

AX-15836 is a potent and selective ERK5 inhibitor with an IC50 of 8 nM.

JWG-071 is a kinase-selective chemical probe targeting ERK5, with an IC50 of 88 nM. It also exhibits inhibitory activity against LRRK2, with an IC50 of 109 nM, making it a valuable tool for studying ERK5- and LRRK2-related signaling pathways.

PROTAC ERK5 degrader-1 is a bifunctional compound designed to target and induce degradation of ERK5 through the VHL-mediated proteasome pathway. Its biological activity has been demonstrated in MOLT-4 cells, highlighting its potential utility in research focused on diseases characterized by dysregulated ERK5 activity, such as acute lymphoblastic leukemia. This reagent is suitable for studies aimed at elucidating the role of ERK5 in various pathophysiological contexts.

ERK5-IN-3 is a potent and selective inhibitor of ERK5 (extracellular signal-regulated kinase 5) with an IC50 of 6 nM. This compound exhibits significant antiproliferative activity against HeLa cells, demonstrating an IC50 of 31 nM. It serves as a valuable tool for investigating the role of ERK5 in cellular signaling pathways and cancer research applications.

(E/Z)-BIX02188 is an inhibitor of the MEK5/ERK5 signaling pathway, targeting the catalytic activity of the MEK5 enzyme. This compound serves as a valuable tool for investigating the role of the MEK5/ERK5 pathway in various biological systems and its implications in cellular processes. Research applications include studying the effects of MEK5/ERK5 modulation in cell growth, differentiation, and response to stress.

JWG-045 is a selective inhibitor of the extracellular signal-regulated kinase 5 (ERK5). In addition to its primary mechanism, JWG-045 displays unique ferroptosis-resistant properties that are independent of ERK5 inhibition. This compound is valuable in breast cancer research, providing insights into ERK5 signaling pathways and their implications in cancer biology.

ERK5-IN-4 is a selective inhibitor of extracellular signal-regulated kinase 5 (ERK5), demonstrating potent activity against both full-length and truncated ERK5 variants. In HEK293 cells, ERK5-IN-4 exhibits inhibitory effects with IC50 values of 77 nM for full-length ERK5 and 300 nM for ERK5 ΔTAD. This compound is valuable for research applications targeting signaling pathways involving ERK5, including studies on cell proliferation, differentiation, and stress response mechanisms.

ERK5-IN-6 is a kinase inhibitor targeting extracellular signal-regulated kinase 5 (ERK5). This compound demonstrates notable anticancer activity, exhibiting an IC50 value of 4.56 µg/mL against A549 lung cancer cells. ERK5-IN-6 is a valuable tool for research into the role of ERK5 in cancer biology and potential therapeutic applications.

ADTL-EI1712 is a selective dual-target inhibitor of ERK1 and ERK5, demonstrating inhibition rates of 93.54% and 89.35%, respectively, at a concentration of 1 μM. It effectively induces regulated cell death by activating genetically encoded machinery, making it valuable for research focused on overcoming compensatory mechanisms in specific cancer cells. This compound is suitable for in vitro and in vivo studies exploring therapeutic strategies targeting the ERK signaling pathway.

PPM-3 is a potent and selective PROTAC degrader of ERK5, exhibiting an IC50 of 62.4 nM. While PPM-3 does not directly affect tumor cell proliferation, it modulates tumor development by impacting macrophage differentiation. This compound may serve as a valuable tool for investigating the role of ERK5 degradation in cancer biology and immune modulation.

ERK5-IN-5 is an inhibitor of the ERK5 kinase, showcasing significant anti-cancer properties. This compound demonstrates notable anti-proliferative effects, with an IC50 value of 6.23 µg/mL against A549 lung cancer cells. ERK5-IN-5 is suitable for research applications focused on cancer biology and signaling pathways involving ERK5 modulation.