Catalog No.
Product Name
Application
Product Information
Citations
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ERK2 inhibitor
TCS ERK 11e (VX-11e) is a potent and selective extracellular signal-related kinase 2 (ERK2) inhibitor (Ki values are <2, 395, 540 and 852 nM for ERK2, GSK-3, Aurora Kinase A and Cdk2 respectively). Potently blocks proliferation of HT29 cells (IC50 = 48 nM).- Bopei Cui, .et al. , Signal Transduct Target Ther, 2023, Sep 25;8(1):366 PMID: 37743418
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ERK1/ERK2 inhibitor
VRT752271 is a pyrrole inhibitors of ERK protein kinase.- Majid Momeny, .et al. , EMBO Mol Med, 2024, Jun 17 PMID: 38886591
- Yuki Shimizu, .et al. , Cancer Lett, 2022, Sep 1;543 PMID: 35724767
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ERK1/RasGAP Inhibitor
The activity of Pluripotin (SC-1) is mediated by the combined inhibition of RasGAP and ERK1 with Kd values of 98 and 212 nM, respectively.- Mohammad Azhar, .et al. , Blood Adv, 2022, Aug 31 PMID: 36044389
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ERK inhibitor
FR 180204 is a novel and selective inhibitor of extracellular signal-regulated kinase (ERK), which may be a potential new therapy for rheumatoid arthritis.- Sergey A Dyshlovoy, .et al. , Sci Rep, 2020, Aug 6;10(1):13178 PMID: 32764580
- Dyshlovoy SA, .et al. , Proteomics, 2017, Jun;17(11) PMID: 28445005
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ERK Inhibitor
SCH772984 is a novel, specific inhibitor of ERK1/2 with IC50 of 4 nM and 1 nM, respectively.- Yuki Shimizu, .et al. , Cancer Lett, 2022, Sep 1;543 PMID: 35724767
- Yajun Li, .et al. , Cell Prolif, 2022, Oct;55(10) PMID: 35708050
- Sergey A. Dyshlovoy, .et al. , Pharmaceuticals, 2021, 14(10), 949 PMID: 34681173
- Sergey A Dyshlovoy, .et al. , Sci Rep, 2020, Aug 6;10(1):13178 PMID: 32764580
- Guo X, .et al. , Pflugers Arch, 2018, Jun;470(6):909-921 PMID: 29441404
- Takuya Hasegawa, .et al. , FEBS Open Bio, 2017, Aug; 7(8): 1154-1165 PMID: 28781955
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food flavouring
2',5'-Dihydroxyacetophenone (DHAP, 2-Acetylhydroquinone, Quinacetophenone) is a mixture of dihydroxyacetophenone isomers is used in food flavouring. 2',5'-Dihydroxyacetophenone significantly inhibits NO production via the suppression of iNOS expression. 2',5'-Dihydroxyacetophenone significantly decreases levels of the pro-inflammatory cytokines TNF-α and IL-6 by blocking the ERK1/2 and NF-κB signaling pathways. -
nAChR agonist
Varenicline Tartrate(CP 526555;Champix) is a nicotinic receptor partial agonist; it stimulates nicotine receptors more weakly than nicotine itself does. - trans-Zeatin is a member of the plant hormone family known as ??cytokinins??, which regulate cell division, development, and nutrient processing.
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ERK1/2 inhibitor
GDC-0994 is a potent and selective Erk1/2 inhibitor. GDC-0994 inhibits both ERK phosphorylation and activation of ERK-mediated signal transduction pathways. -
ERK5 inhibitor
XMD17-109 is a novel, specific inhibitor of ERK-5 with an EC50 value of 4.2 uM in HEK293 cells. - 4-Methylbenzylidene camphor(4-MBC; Enzacamene)is an organic camphor derivative that is used in the cosmetic industry for its ability to protect the skin against UV, specifically UV B radiation.
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ERK/Akt/NF-kB inhibitor
Tomatidine inhibits the phosphorylation of ERK, Akt, and the nuclear content of NF-kB. possess anti-inflammatory properties. -
ERK inhibitor
MK-8353 (SCH900353) is an orally bioavailable, selective, and potent ERK inhibitor that inhibits activated ERK1 and ERK2 in vitro, with IC50 values of 23.0 nM and 8.8 nM, respectively (IMAP kinase assay), and nonactivated ERK2, with an IC50 of 0.5 nM (MEK1-ERK2-coupled assay). -
ERK inhibitor
AZD0364 is a pre-clinical ERK1/2 inhibitor with an IC50 of 0.6 nM for ERK2. -
ERK inhibitor
LY3214996 is a selective and novel ERK1/2 inhibitor with IC50 of 5 nM for both enzymes in biochemical assays. It potently inhibits cellular phospho-RSK1 in BRAF and RAS mutant cancer cell lines. - Omtriptolide (PG490-88) is a water soluble derivative prodrug of triptolide purified from the Chinese herb
- Xanthocillin is a marine agent extracted from Penicillium commune, induces autophagy through inhibition of the MEK/ERK pathway.
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RAF/ERK1/2 inhibitor
Rineterkib (ERK-IN-1) (compound B) is a RAF and ERK1/2 inhibitor in the treatment of a proliferative disease characterized by activating mutations in the MAPK pathway.
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ERK1/2 inhibitor
ERK1/2 inhibitor 1 is a potent, orally bioavailable ERK1/2 inhibitor, showing 60% inhibition at 1 nM and an IC50 of 3.0 nM against ERK1 and ERK2, respectively. -
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. -
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. -
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. -
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. -
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.
