ERK

ERK1/2 inhibitor 8 is a potent inhibitor of extracellular signal-regulated kinases (ERK) with an IC50 value of 0.48 nM specifically targeting ERK2. This compound is valuable for research applications involving cellular signaling pathways, especially those related to cancer and inflammation. Its high potency makes it an essential tool for elucidating ERK-mediated biological processes and developing therapeutic strategies.

ERK2/p38α MAPK-IN-1 is a selective inhibitor targeting ERK2 and p38α MAPK, exhibiting an IC50 of 82 μM for ERK2. This compound binds allosterically to both ERK2 and p38α MAPK, influencing their activity through distinct mechanisms. It is primarily utilized in research concerning type 2 diabetes, contributing to studies aimed at understanding the molecular pathways involved in this condition.

ERK1/2 Inhibitor 4 is a selective inhibitor targeting the extracellular signal-regulated kinases 1 and 2 (ERK1/2), key components of the mitogen-activated protein kinase (MAPK) signaling pathway. This compound exhibits potent inhibition of ERK1/2 activity, making it a valuable tool for studying cellular signaling and its implications in cancer, inflammatory responses, and various proliferative disorders. Research applications include elucidating the role of ERK1/2 in tumorigenesis and exploring therapeutic strategies in related diseases.

STE-MEK1(13) is a selective inhibitor of the ERK1/2 pathway, effectively blocking the phosphorylation of both ERK1 and ERK2. With an IC50 range of 13-30 μM, this cell-permeable compound is valuable for investigating the role of ERK signaling in cellular processes. Applications include studies on cancer biology, cell proliferation, and differentiation, making it a useful tool for researchers exploring MAPK pathway modulation.

ERK-IN-2 free base is a selective inhibitor of ERK2, demonstrating an IC50 value of 1.8 nM. This compound is useful for studying the role of ERK2 in various signaling pathways and cellular processes. Researchers should be mindful of potential off-target toxicity or activity at concentrations exceeding 10 μM, which may impact experimental outcomes.

ERK-IN-8 is an aniline pyrimidine derivative that functions as a selective inhibitor of ERK2. It demonstrates potent inhibitory activity with an IC50 of ≤50 nM in vitro. This compound is valuable for applications in cancer research, enabling investigations into ERK signaling pathways and their roles in tumorigenesis.

Laxiflorin B is a selective inhibitor of ERK1/2, a key component of the MAPK signaling pathway. It exhibits significant antitumor activity, making it a valuable compound for cancer research. Laxiflorin B is particularly useful for investigations into the molecular mechanisms of ERK-related pathways and their roles in oncogenesis.

ERK2 IN-5 is a selective inhibitor of ERK2 that demonstrates significant affinity for the target, with a Ki value of 86 nM, as well as for JNK3, with a Ki of 550 nM. This compound is suitable for research applications involving the modulation of ERK signaling pathways, providing a valuable tool for studying cellular processes such as proliferation, differentiation, and apoptosis in various biological contexts.

ERK2-IN-3 is a selective inhibitor of ERK2, effectively blocking the phosphorylation of both Erk2WT and Erk2DS1 activation loops with IC50 values of 5 μM and 42 nM, respectively. This compound provides valuable insights into the role of ERK2 in various signaling pathways and is applicable in research related to cancer, cell proliferation, and differentiation. ERK2-IN-3 may facilitate the study of ERK signaling and its potential therapeutic interventions.

ERK1/2 Inhibitor 5 is a highly effective inhibitor specifically targeting ERK1/2, members of the mitogen-activated protein kinase (MAPK) family. By interfering with the MAPK signaling pathway, this compound demonstrates significant potential in research applications related to cancer, inflammation, and other proliferative disorders. Its ability to modulate cellular signaling makes it a valuable tool in the study of various pathophysiological conditions.

β-Neo-Endorphin acetate is an endogenous opioid peptide that primarily acts as an Erk1/2 activator. Originating from porcine hypothalamus as a precursor to Leu-enkephalin, it demonstrates significant biological activity by activating Erk1/2, as well as matrix metalloproteinases MMP-2 and MMP-9. This compound is valuable for research focused on neurobiology, pain modulation, and cellular signaling pathways involving opioid receptors.

ERK2 allosteric-IN-1 is a selective allosteric inhibitor of ERK2, exhibiting an IC50 value of 11 μM. This compound modulates ERK2 activity, providing a valuable tool for investigating the role of ERK1/2 signaling in various biological processes. Its specificity for ERK2 makes it suitable for studies in cancer research, cellular signaling, and related therapeutic applications.

OP-1118 is a potent dual inhibitor of NF-κB and ERK1/2, targeting critical signaling pathways involved in inflammation and cell survival. This compound demonstrates significant anti-inflammatory, cytoprotective, anti-apoptotic, and antibacterial activities by inhibiting the phosphorylation of NF-κB and ERK1/2, leading to a reduction in pro-inflammatory cytokine expression. In preclinical models of Clostridium difficile infection, OP-1118 effectively mitigates toxin-induced intestinal inflammation, cellular damage, and apoptosis, with its protective effects possibly reversible by PMA. This makes OP-1118 a valuable reagent for research into inflammatory conditions and therapeutic interventions.

Laxiflorin B-4 is a selective ERK1/2 inhibitor, demonstrating a higher affinity compared to its parent compound, Laxiflorin B. This enhanced binding significantly increases its potential for tumor suppression, making it a valuable tool in cancer research. Laxiflorin B-4 can aid in the study of ERK signaling pathways and their role in oncogenesis.

Picrasidine J is a selective inhibitor of KLK-10 protease and the ERK signaling pathway. It demonstrates significant anti-migratory and anti-invasive activities by upregulating E-Cadherin and ZO-1 while downregulating β-catenin and Snail. Additionally, it reduces KLK-10 expression and inhibits ERK phosphorylation. Picrasidine J is primarily utilized in research aimed at preventing metastasis in head and neck squamous cell carcinoma (HNSCC).

ERK1/2 inhibitor 6 is a selective inhibitor targeting extracellular signal-regulated kinases 1 and 2 (ERK1/2), key components of the mitogen-activated protein kinase (MAPK) signaling pathway. This compound exhibits significant activity in modulating signal transduction processes, making it a valuable tool in cancer research, inflammation studies, and the investigation of other proliferative diseases. Its potential applications include elucidating the role of ERK1/2 in cellular processes and exploring therapeutic strategies for related pathologies.

Sonvuterkib is a potent inhibitor of extracellular signal-regulated kinases (ERK), demonstrating IC50 values of 1.4 nM for ERK1 and 0.54 nM for ERK2. This orally active compound effectively inhibits cell proliferation, making it a valuable tool in cancer research. Its ability to target ERK signaling pathways highlights its potential for therapeutic applications in various cancer models.

ITZ-1 is a selective inhibitor of the extracellular signal-regulated kinase (ERK) in the mitogen-activated protein kinase (MAPK) pathway, exhibiting an IC50 of 0.51 μM against interleukin-1β (IL-1β)-induced matrix metalloproteinase-13 (MMP-13) production. This compound effectively reduces MMP-13 expression and mitigates nitric oxide (NO)-induced chondrocyte apoptosis. ITZ-1 holds potential for advancing research in osteoarticular diseases.

ERK1/2 inhibitor 10 is a highly potent inhibitor of ERK1 and ERK2, exhibiting IC50 values of 0.11 nM and 0.08 nM, respectively. This compound effectively blocks the phosphorylation of downstream substrates, including p90RSK and c-Myc, leading to enhanced cell apoptosis and incomplete autophagy-related cell death. ERK1/2 inhibitor 10 demonstrates significant antitumor activity against triple-negative breast cancer and colorectal cancer models, particularly those with BRAF and RAS mutations, making it a valuable tool for cancer research.

ERK1/2 Inhibitor 12 is a selective inhibitor of the ERK1 and ERK2 signaling pathways. It effectively inhibits ERK-mediated phosphorylation of caspase-9 and p90Rsk-1 kinase, demonstrating significant anti-cancer activity. This compound is suitable for research applications focused on cancer biology and the modulation of ERK signaling in various cellular contexts.

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.

Fulipiftide is a short peptide that acts as an activator of the ERK2 and STAT3 signaling pathways. This compound promotes the expansion of nuclear stem cell factor +TSPC, demonstrating significant anti-inflammatory activity. Fulipiftide is particularly useful in research related to acute tendon injury and in studies exploring regenerative medicine and tissue repair mechanisms.

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.

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.

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.