MAPK
Catalog No.
Product Name
Application
Product Information
Citations
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p38 MAPK Activator
Iroxanadine hydrochloride is a dual activator of p38 mitogen-activated protein kinase (MAPK) and heat shock proteins (HSPs). It exhibits vasculoprotective properties, making it a valuable tool for investigating mechanisms underlying atherosclerosis and various vascular diseases. This reagent is suitable for research applications focused on the modulation of inflammatory responses and cellular stress pathways. -
p38 MAPK Activator
Iroxanadine hydrobromide is a potent activator of p38 MAPK and HSP proteins. This compounds biological activity focuses on vasculoprotection, making it a valuable tool for investigating atherosclerosis and other vascular diseases. Its dual activation mechanisms provide insights into cellular stress responses and inflammation, making it relevant for research applications in cardiovascular health. -
p38 MAPK Activator
Iroxanadine is a dual activator of p38 MAPK and heat shock proteins (HSPs). It exhibits vasculoprotective properties, making it a valuable reagent for studying atherosclerosis and other vascular diseases. This compound can be utilized in research focusing on inflammatory responses and cardiovascular health, providing insights into the mechanisms underlying these conditions. -
PROTAC ERK5 Degrader
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. -
ERK Inhibitor
Enniatin B is an ERK inhibitor derived from the Fusarium species. This mycotoxin demonstrates significant inhibition of acyl-CoA:cholesterol acyltransferase (ACAT) with an IC50 value of 113 μM, as observed in enzyme assays utilizing rat liver microsomes. Enniatin B effectively reduces the activation of ERK (p44/p42), making it a valuable tool for research focused on signal transduction pathways and their implications in various biological processes. -
MEK1/MEK2 Inhibitor
IK-595 is a selective inhibitor of MEK1 and MEK2, exhibiting a high binding affinity of 7.39 nM. It effectively blocks EGF-induced phosphorylation of ERK1/2 in AsPC-1 cells, with an IC50 of 0.1 nM. Notably, IK-595 demonstrates oral bioavailability and the ability to penetrate the blood-brain barrier, making it a valuable tool for investigating Ras/MAPK pathway-altered cancers. -
PROTAC MEK1 Inhibitor
PROTAC MEK1 Degrader-1 is a targeted protein degradation compound that selectively degrades MEK1 via a PROTAC mechanism. With a pIC50 value of 7.0, it effectively inhibits ERK1/2 phosphorylation, leading to downstream signaling modulation. This compound demonstrates significant antiproliferative activity against A375 melanoma cells, making it a valuable tool for research in cancer therapeutics and signaling pathway studies. -
ERK2 Inhibitor
(R)-VX-11e is a selective inhibitor of the extracellular signal-regulated kinase 2 (ERK2), a key component of the MAPK signaling pathway. This compound has been shown to effectively interfere with ERK2-mediated signal transduction, leading to alterations in cell proliferation and differentiation. It serves as a valuable tool in cancer research by elucidating the role of ERK2 in tumor progression and therapeutic response. -
ERK2 Inhibitor
ERK-IN-2 is a potent ERK2 inhibitor with an IC50 of 1.8 nM, demonstrating strong selectivity for its target. This compound effectively modulates ERK2 activity, which is critical in various signaling pathways related to cell growth, proliferation, and survival. ERK-IN-2 is well-suited for research applications investigating ERK signaling in cancer and other diseases, though caution is advised regarding potential off-target effects at doses exceeding 10 μM. -
ERK1/2 Inhibitor
ERK1/2 Inhibitor 3 is a selective inhibitor of ERK1/2, members of the mitogen-activated protein kinase (MAPK) family, which are critical components in cellular signal transduction pathways. This compound demonstrates significant potential in the study of cancer, inflammation, and other proliferative diseases due to its ability to modulate ERK signaling. Research applications include elucidating the role of ERK1/2 in various pathological conditions and exploring therapeutic strategies targeting aberrant MAPK activity. -
ROCK/ERK/GSK/AGC Inhibitor
ROCK-IN-5 (compound I-B-37) is a potent inhibitor of Rho-associated protein kinase (ROCK), as well as ERK, GSK-3, and AGC protein kinases. This compound exhibits significant biological activity in regulating cellular proliferation and has applications in researching cardiac conditions and neurodegenerative diseases. Its broad inhibitory profile makes it a valuable tool for studies aimed at understanding signaling pathways involved in various disease mechanisms. -
ERK1/2 Inhibitor
MK-8353 hydrochloride is a selective inhibitor of ERK1/2, demonstrating IC50 values of 23.0 nM and 8.8 nM for each target, respectively. This compound shows significant antitumor activity, making it a valuable tool for cancer research. Its oral bioavailability allows for convenient administration in preclinical studies focused on the MAPK signaling pathway and its role in tumor progression. -
ERK5 Inhibitor
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. -
PKCδ/ERK Signaling Pathway Protein
PKCδ substrate is a selective target for protein kinase C delta (PKCδ), functioning primarily as a nuclear transporter for ERK2. It plays a crucial role in ERK2-mediated gene activation and is involved in regulating various cellular processes, including growth, proliferation, cell cycle arrest, and apoptosis through the phosphorylation of hBVR and additional substrates. This reagent is essential for studying the mechanisms underlying disease development, particularly in cancer biology and related signaling pathways. -
PI3K/AKT/ERK/CREB Activator
PI3K/AKT/ERK/CREB Activator 1 is a small molecule that stimulates the PI3K/AKT/ERK/CREB signaling pathway. It enhances neuronal survival and proliferation, promoting the viability of damaged neurons and facilitating synapse formation. This compound also reduces neuroinflammation by decreasing pro-inflammatory cytokine levels, and it has shown potential in preserving synaptic structure and improving spatial memory in Alzheimer's disease models. PI3K/AKT/ERK/CREB Activator 1 is a valuable tool for research focused on neurodegenerative disorders, particularly Alzheimer's disease. -
MEK5/ERK5 Inhibitors
(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. -
ERK2 Inhibitor
TAT-MEK1 is an ERK2 inhibitor that combines the TAT peptide with the N-terminal region of MEK1, enabling efficient cellular uptake. This compound exhibits an in vitro IC50 of 29 μM for ERK2, demonstrating its potent inhibitory action. TAT-MEK1 is primarily utilized in research to investigate ERK2-related signaling pathways and explore its implications in various cellular processes and disease states. -
SOS1 Activator
SOS1 Activator 2 engages the SOS1 protein, functioning as a potent activator with a binding affinity characterized by a Kd of 9 nM. By modulating the Ras-ERK signaling pathway, SOS1 Activator 2 serves as a valuable tool in cancer research, facilitating investigations into signal transduction mechanisms and potential therapeutic strategies. Its specificity and efficacy make it an essential reagent for studies aimed at understanding the complexities of oncogenic signaling pathways. -
ERK5 Inhibitor
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. -
ERK Inhibitor
ERK-IN-7 is a potent inhibitor of extracellular signal-regulated kinases 1 and 2 (ERK1/ERK2), exhibiting IC50 values of 5 nM and 7 nM, respectively. This compound is designed for research applications targeting ERK signaling pathways, which are critical in cell proliferation, differentiation, and survival processes. ERK-IN-7 serves as a valuable tool for investigating the role of ERK in various biological contexts and therapeutic strategies in cancer and other diseases. -
ERK Inhibitor
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 Inhibitor
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
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. -
ERK1/2 Inhibitor
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. -
ERK2 Inhibitor
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 Inhibitor
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. -
SOS1-Ras Inhibitor
UC-857993 is a selective inhibitor of the SOS1-Ras interaction, effectively suppressing its catalytic activity with a Kd of 14.7 μM (His6-SOS1cat). This compound also inhibits ERK and Ras activation, demonstrating significant capabilities in reducing the proliferation of mouse embryonic fibroblasts (MEFs). UC-857993 is valuable for research into cancer biology and signaling pathways involving Ras. -
ERK Inhibitor
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. -
ERK Inhibitor
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 Inhibitor
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
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. -
Erk1/2 Activator
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 Inhibitor
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. -
NF-κB&ERK1/2 Inhibitor
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. -
ERK Inhibitor
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. -
KLK-10/ERK Inhibitor
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
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. -
ERK Inhibitor
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. -
ERK-MAPK Pathway Inhibitor
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
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
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 Inhibitor
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 Inhibitor
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. -
Erk2 Inhibitor
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. -
ERK2 Inhibitor
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. -
BRAF PROTACs Negative Control
CG 858-Neg is a negative control for Thalidomide-derived PROTAC degraders targeting BRAF and BRAFV600E, exhibiting Ki values of 9.5 nM and 14.4 nM, respectively. This compound effectively inhibits downstream phosphorylation of ERK and demonstrates suppression of BRAFV600E-driven tumorigenesis in melanoma (A375 cells, IC50 = 492 nM) and colorectal cancer (HT-29 cells, IC50 = 459 nM) models. CG 858-Neg is suitable for research applications focused on the mechanisms of melanoma and colorectal carcinoma. -
ERK1/5 Inhibitor
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. -
Selective p38α Inhibitor
AMG-548 dihydrochloride is a selective p38α inhibitor with a Ki of 0.5 nM, exhibiting moderate selectivity towards p38β (Ki = 36 nM) and over 1000-fold selectivity against p38γ and p38δ isoforms. This compound demonstrates potent inhibition of TNFα production in whole blood stimulated by LPS, with an IC50 of 3 nM. Additionally, AMG-548 dihydrochloride inhibits Wnt signaling by directly targeting Casein kinase 1 isoforms δ and ε, making it valuable for research in inflammation and signaling pathways. -
Selective p38α Inhibitor
AMG-548 hydrochloride is a selective inhibitor targeting p38α with a Ki of 0.5 nM and shows moderate selectivity for p38β (Ki=36 nM), while exhibiting over 1000-fold selectivity against p38γ and p38δ. This compound effectively inhibits TNFα production in whole blood stimulated by LPS, with an IC50 of 3 nM. Additionally, AMG-548 hydrochloride disrupts Wnt signaling through the direct inhibition of Casein kinase 1 isoforms δ and ε, making it a valuable reagent for studies in inflammation and cancer research. -
p38/CK1 Inhibitor
p38α inhibitor 8 selectively inhibits p38α MAPK and CK1δ, with IC50 values of 0.21 µM and 0.202 µM, respectively. This compound is valuable for studies exploring cellular stress responses and inflammatory pathways, making it a potent tool in cancer research and immunology. Its ability to modulate these kinases presents opportunities for investigating therapeutic strategies in various diseases.
