Shop By
Catalog No.
Product Name
Application
Product Information
Citations
-
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
-
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
-
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
-
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
-
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
-
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. -
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. -
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.
-
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. -
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. -
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. -
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. -
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. -
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. -
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.
