ERK

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.

ETP-45835 dihydrochloride is a selective inhibitor of Erk2, exhibiting an IC50 value of 18.7 μM. This compound demonstrates significant inhibitory effects on cell proliferation, with an EC50 value of 0.9 μM. ETP-45835 is valuable for research applications focused on cell signaling pathways and the modulation of Erk2 activity in various biological contexts.

Tizaterkib (hexanedioic acid) is a potent and selective inhibitor of ERK2, exhibiting an IC50 of 0.6 nM. This compound effectively disrupts ERK2 signaling pathways, making it valuable for investigating the role of ERK2 in various biological processes. Its application extends to cancer research and drug discovery, providing insights into therapeutic strategies targeting ERK2-associated pathways.

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.

Methyllinderone is an inhibitor of the AP-1, STAT, and ERK signaling pathways. This compound exhibits anti-inflammatory properties and has been shown to reduce the invasion and migration rates of TPA-stimulated MCF-7 breast cancer cells. Methyllinderone serves as a valuable tool for research applications focused on breast cancer metastasis and the underlying mechanisms of cancer progression.

Ulixertinib hydrochloride is a potent, orally active inhibitor of the ERK1/2 kinases, functioning primarily through ATP competition and reversible covalent binding. With an IC50 of less than 0.3 nM against ERK2, this compound effectively inhibits phosphorylated ERK2 (pERK) and its downstream target, RSK (pRSK) in A375 melanoma cells. Ulixertinib hydrochloride is valuable for research aimed at understanding the role of ERK signaling in cancer biology and therapeutic strategies targeting this pathway.

Ravoxertinib hydrochloride is an orally bioavailable inhibitor that selectively targets ERK kinase activity, demonstrating IC50 values of 6.1 nM for ERK1 and 3.1 nM for ERK2. This compound exhibits significant inhibition of ERK signaling pathways, making it a valuable tool for research in cancer biology and targeted therapies. Its selective action on ERK kinases positions it as an important reagent for investigating therapeutic strategies in ERK-driven malignancies.

ZINC12409120 is a highly selective ERK inhibitor that targets the mitogen-activated protein kinase pathway. It disrupts the interaction between FGF23 and α-Klotho, leading to inhibition of ERK activity with an IC50 of 5.0 μM. This compound is valuable for research applications focused on cellular signaling pathways and their implications in various disease models.

ERK1/2 Inhibitor 9 is a covalent inhibitor targeting ERK1/2, exhibiting sub-micromolar activity in cellular assays with a GI50 of 0.47 μM in A375 cells. This compound effectively downregulates phospho-ERK1/2 levels, thereby impacting downstream signaling pathways. Additionally, ERK1/2 Inhibitor 9 is functionalized with trans-cyclo-octene (TCO) and Tz-Thalidomide, enabling the formation of ERK-CLIPTAC for targeted degradation of ERK1/2. This makes it a valuable tool for research into cancer signaling mechanisms and targeted protein degradation strategies.

Ambuic acid is a potent inhibitor targeting the ERK/JNK pathway, demonstrating notable anti-inflammatory effects. It displays significant antimicrobial activity against Staphylococcus aureus, with an IC50 value of 43.9 μM for the ATCC 6538 strain. Additionally, Ambuic acid inhibits the biosynthesis of cyclic peptide quorum sensing molecules in gram-positive bacteria, making it a valuable compound for research in antimicrobial and anti-inflammatory applications.

ERK2-IN-4 is a selective inhibitor of the ERK2 pathway, demonstrating a Ki of 0.006 μM. This compound effectively disrupts ERK signaling, making it a valuable tool in cancer research. Its specificity and potency allow for detailed studies of ERK2's role in tumorigenesis and related signaling pathways.

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.

ERK Inhibitor II (Negative Control) is a selective inhibitor of extracellular signal-regulated kinase (ERK) primarily affecting the insulin receptor pathway. This compound serves as a tool for investigating the role of ERK in various biological processes, particularly in the research of diabetes and insulin signaling mechanisms. Its application extends to studying the modulation of ERK activity and understanding associated cellular responses.

Methyl helicterate is a triterpenoid compound that functions as an inhibitor of the ERK1/2 signaling pathway. It demonstrates significant biological activity by inhibiting hepatic stellate cell activation and promoting apoptosis in these cells. This manipulation of the ERK1/2 pathway positions methyl helicterate as a valuable reagent for research focused on liver fibrosis and related conditions.

ERK1/2 inhibitor 13 is a potent dual inhibitor of ERK1 and ERK2, exhibiting IC50 values of 91.71 nM and 97.87 nM, respectively. This compound demonstrates significant activity in inhibiting the proliferation of tumor cell lines, including MCF-7, 4T1, MDA-MB-468, and HCC1970, with IC50 values ranging from 0.67 to 2.76 μM. Additionally, ERK1/2 inhibitor 13 effectually inhibits cancer cell migration and induces apoptosis and autophagy in MCF-7 cells, while also displaying antitumor and anti-metastatic properties in a 4T1 xenograft mouse model, making it a valuable reagent for cancer research applications.

SF-3-030 is a selective, non-ATP competitive inhibitor of ERK1/2, targeting the MAPK signaling pathway. It has demonstrated the ability to induce apoptosis specifically in melanoma cells with mutated BRAF and activated ERK1/2 signaling. Additionally, SF-3-030 has shown potential in alleviating several characteristics of asthma in murine models, making it valuable for research focused on both melanoma and asthma pathophysiology.