MAPK
Catalog No.
Product Name
Application
Product Information
Citations
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Mnk2/JAK3 inhibitor
Cercosporamide, an usnic amide, was originally identified in Cercosporidium henningsii as a host-selective phytotoxin and broad-spectrum antifungal agent and is a potent inhibitor of MAP-kinase interacting kinase-2 (Mnk2; IC50 = 11 nM), JAK3 (IC50 = 31), and Mnk1 (IC50 = 116 nM). -
p38 MAPK inhibitor
SB 203580 hydrochloride (Adezmapimod hydrochloride) (RWJ 64809 hydrochloride) is a widely used p38 MAPK inhibitor.
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MAPKAPK2(MK2) inhibitor
MK2-IN-1 hydrochloride is a potent and selecitve MAPKAPK2(MK2) inhibitor(IC50=0.11 uM) with a non-ATP competitive binding mode. -
ALK/MET inhibitor
Ensartinib hydrochloride (X-396 hydrochloride) is a potent and dual ALK/MET inhibitor with IC50s of <0.4 nM and 0.74 nM, respectively. -
JNK Acticator
Juglanin is a naturally occurring flavonoid isolated from Polygonum aviculare, primarily acting as a JNK activator. It exhibits significant anti-inflammatory, antioxidant, and antitumor properties. Research indicates that Juglanin induces apoptosis and promotes autophagy in human breast cancer cells, making it a valuable reagent for studies on cancer biology and therapeutic interventions. -
JNK Activator
BDE 47 is a JNK activator that targets mitochondria to inhibit mitochondrial oxidative phosphorylation (OXPHOS). This compound decreases mitochondrial membrane potential (MMP) and induces apoptosis in embryonic cells. Additionally, BDE 47 triggers the generation of reactive oxygen species (ROS) and activates the JNK signaling pathway, demonstrating embryonic developmental toxicity in zebrafish models. Its unique properties make it a valuable tool for research on oxidative stress and developmental biology. -
NF-κB Expression Reducer, ERK 1/2 Activator, Beta-Adrenergic Receptor Modulator, Calcium Channel Inhibitor
Eupatorin is a flavonoid that functions primarily as an NF-κB expression reducer and an ERK 1/2 activator, while also modulating beta-adrenergic receptors and inhibiting calcium channels. It demonstrates significant antiproliferative and vasodilatory effects, inducing apoptosis and causing G2/M phase cell cycle arrest, alongside reactive oxygen species (ROS) production. Eupatorin has been shown to impact inflammatory mediators and calcium signaling pathways, making it relevant for research in breast cancer, hypertension, and leukemia. Metabolized by CYP1A1 and other CYP1 enzymes, Eupatorin yields bioactive metabolites that maintain antiproliferative properties. -
Rb-Raf-1 Inhibitor
RRD-251 is a selective inhibitor of the retinoblastoma tumor suppressor protein (Rb)-Raf-1 interaction. This compound exhibits potent anti-proliferative, anti-angiogenic, and anti-tumor activities, making it valuable for research focused on cancer biology and therapeutic strategies targeting cell growth and tumor progression. Its ability to disrupt this critical protein interaction highlights its potential use in studies investigating the molecular mechanisms underlying various cancers. -
p38 MAPK Activator
MTBT is a p38 MAPK activator with notable anticancer properties. It effectively inhibits tumor cell proliferation, inducing cell cycle arrest and apoptosis. MTBT enhances the phosphorylation of histone H3 at serine residues in cancer cells, thereby facilitating cell cycle arrest in the M phase. The specific p38 MAPK inhibitor Adezmapimod can reverse the cell cycle arrest effects initiated by MTBT, making it a valuable tool in cancer research and therapeutic studies. -
p38 MAPK Agonist
4-Hydroxylonchocarpin is a chalcone compound that acts as an agonist of p38 MAPK. This reagent enhances the phosphorylation of p38 MAPK, JNK, and ERK pathways, thereby promoting the induction of reactive oxygen species (ROS) and apoptosis in liver cancer cells. Additionally, 4-Hydroxylonchocarpin exhibits a diverse range of pharmacological activities, including antibacterial, anticancer, anti-retroviral, anti-tuberculosis, anti-malarial, and anti-inflammatory effects, making it a valuable tool for various research applications in cancer and infectious disease studies. -
GCK/MAP4K2 Inhibitor
TL4-12 is a selective inhibitor of MAP4K2 and GCK, demonstrating a dose-dependent ability to downregulate IKZF1 and BCL-6. This compound effectively inhibits cell proliferation in multiple myeloma with an IC50 of 37 nM, and it also induces apoptosis in cancerous cells. TL4-12 holds potential for overcoming resistance to immunomodulatory agents in the treatment of multiple myeloma. -
JNK Inhibitor
JNK-IN-17 is a selective and potent inhibitor of c-Jun N-terminal kinase (JNK), demonstrating IC50 values of 0.039 μM and 0.079 μM for JNK1 and JNK3, respectively. It effectively inhibits c-Jun phosphorylation with an IC50 of 0.082 μM in Streptozotocin-induced INS-1 pancreatic islet β cells. Additionally, JNK-IN-17 exhibits low interaction potential, showing an inhibition rate of ≤ 33% on major cytochrome P450 subtypes in human liver microsomes. This compound is valuable for research applications related to neurological and metabolic disorders, including Parkinson's disease. -
FGFR3/BRAF Binder
2,4,3',4',6'-Penta-O-(3-methylbutanoyl)sucrose functions as a selective binder for Fibroblast Growth Factor Receptor 3 (FGFR3) and BRAF, playing a pivotal role in modulating pathways associated with cancer progression. Derived from Atractylodes japonica, this compound exhibits low cytotoxicity towards cancer cell lines, making it a suitable candidate for research applications focused on targeted cancer therapies and signaling pathway studies. Its unique structural characteristics enhance its potential for further exploration in drug development and therapeutic interventions. -
TAK1 Inhibitor
SM1-71 is a potent TAK1 inhibitor exhibiting a Ki value of 160 nM. It targets multiple kinases, including MKNK2, MAP2K1/2/3/4/6/7, and GSK3A/B, among others, providing a broad scope of biological activity. This compound has demonstrated the ability to inhibit the proliferation of various cancer cell lines, making it a valuable tool for cancer research and therapeutic development. -
RAF Inhibitor
CCT241161 is a potent pan-RAF inhibitor that effectively targets multiple RAF family members with IC50 values of 3 nM for LCK, 6 nM for CRAF, 10 nM for SRC, 15 nM for V600E-BRAF, and 30 nM for BRAF. This compound demonstrates significant antiproliferative activity in BRAF and NRAS mutant melanoma cell lines, making it a valuable tool for cancer research. CCT241161 is relevant for studies focused on targeted therapies in oncogenic signaling pathways. -
p38/JNK Inhibitor
LL-Z1640-4 is a selective inhibitor of p38 and JNK signaling pathways, demonstrating significant efficacy in attenuating their activation in hepatocellular carcinoma (HCC) cells following MLK4 siRNA transfection. This compound effectively reduces reactive oxygen species (ROS) production associated with MLK4 knockdown and subsequently decreases apoptosis in these HCC cells. LL-Z1640-4 serves as a valuable tool for investigating the roles of p38 and JNK in cancer biology and therapeutic interventions. -
ERK-MYD88 Interaction Inhibitor
ERK-MYD88 Interaction Inhibitor 1 specifically targets the interaction between ERK and MYD88. This compound promotes an integrated stress response mediated by HRI, resulting in immunogenic apoptosis within cancer cells. In preclinical studies, ERK-MYD88 Interaction Inhibitor 1 has demonstrated the ability to stimulate anti-tumor T cell responses in Lewis lung cancer mouse models, showcasing its potential as an anti-tumor agent. -
TOPK Inhibitor
OTS964 is a selective inhibitor of T-cell orientation protein kinase (TOPK), demonstrating a high affinity with an IC50 of 28 nM. Additionally, OTS964 effectively inhibits cyclin-dependent kinase 11 (CDK11), with a binding affinity (Kd) of 40 nM for CDK11B. This compound is utilized in research exploring cancer therapeutic strategies and cell cycle regulation. -
MEK Inhibitor
MEK-IN-5 is a potent inhibitor of the MEK pathway, functioning by significantly decreasing the phosphorylation levels of MEK and ERK in a dose-dependent and time-dependent manner. In addition to its inhibitory effects on MEK signaling, MEK-IN-5 acts as a nitric oxide donor, contributing to its biological activity. This compound has been shown to induce apoptosis in MDA-MB-231 breast cancer cells, making it a valuable tool for research in cancer therapeutics and signaling pathways. -
p38 MAPK Ihibitor
SB 202190 hydrochloride is a selective inhibitor of the p38 MAP kinase with IC50 values of 50 nM and 100 nM for p38α and p38β, respectively. By binding to the ATP pocket of active recombinant human p38 kinase with a Kd of 38 nM, it demonstrates significant anti-cancer activity. Furthermore, SB 202190 hydrochloride has been shown to induce autophagy, making it a valuable tool for research in cancer biology and signaling pathways related to stress response. -
p38 MAPK Inhibitor
FR 167653 is a selective inhibitor of p38 mitogen-activated protein kinase (MAPK), demonstrating significant suppression of pro-inflammatory cytokines such as TNF-α and IL-1β through targeted inhibition of p38 MAPK activity. This compound is effective in preclinical models for managing inflammation and provides therapeutic benefits in conditions related to trauma and ischemia-reperfusion injury. Its ability to modulate inflammatory responses makes it a valuable tool for research in inflammation and related disorders. -
p38 MAPK Inhibitor
Dilmapimod tosylate is a potent inhibitor of p38 mitogen-activated protein kinase (MAPK), a key regulator of inflammatory responses. This compound exhibits significant biological activity by reducing pro-inflammatory cytokine production, making it a valuable tool in studying inflammatory processes. It has potential applications in researching chronic inflammatory diseases, including chronic obstructive pulmonary disease (COPD). -
p38 MAPK Inhibitor
p38 MAPK-IN-2 is a selective inhibitor of p38 mitogen-activated protein kinase (MAPK). This compound effectively attenuates p38 MAPK signaling, leading to decreased phosphorylation of downstream targets involved in inflammatory responses. It is valuable for researchers studying cellular stress responses, cytokine signaling, and potential therapeutic effects in various inflammatory diseases and cancer. -
p38 MAPK Inhibitor
2-Phenylacetamide is a potent inhibitor of the p38 MAPK signaling pathway. This compound demonstrates significant anti-inflammatory, antioxidant, anti-hypertensive, and anti-fibrotic properties, making it a valuable tool for investigating various biological processes. Additionally, 2-Phenylacetamide is orally active, facilitating its use in in vivo research applications. -
JNK Inhibitor
JNK-9L is an ATP-competitive inhibitor targeting c-Jun N-terminal kinases (JNK1 and JNK3), exhibiting IC50 values of 0.099 and 0.148 μM, respectively. This compound effectively inhibits c-jun phosphorylation and reduces reactive oxygen species (ROS) generation induced by Streptozotocin with an IC50 of 0.8 nM. JNK-9L is particularly relevant for research into neurodegenerative diseases, including Parkinson’s disease, facilitating investigations into the therapeutic modulation of JNK pathways. -
p38 Kinase/HSP Activator
(±)-Iroxanadine serves as a p38 kinase and heat shock protein (HSP) activator, demonstrating vasculoprotective properties. This compound is pertinent for research into atherosclerosis and various vascular diseases, facilitating studies aimed at understanding the molecular mechanisms underlying these conditions. Its activation of key signaling pathways makes it a valuable tool for exploring therapeutic targets in cardiovascular research. -
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.
