MAPK
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Catalog No.
Product Name
Application
Product Information
Citations
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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. -
p38-α MAPK inhibitor
5,6,7-Trimethoxyflavone is a novel p38-α MAPK inhibitor with an anti-inflammatory effect. 5,6,7-Trimethoxyflavone is isolated from several plants including Zeyhera tuberculosa, Callicarpa japonica, and Kickxia lanigera. -
MNK1/MNK2 inhibitor
Tomivosertib (eFT508) is a potent, highly selective, and orally bioavailable MNK1 and MNK2 inhibitor, with IC50s of 1-2 nM against both isoforms. -
SOS1 inhibitor
BI-3406 (SOS1-IN-2) is a Son of Sevenless 1 (SOS1) inhibitor with an IC50 of 6 nM.
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Raf nhibitor
RAF mutant-IN-1 is a RAF kinase inhibitor, extracted from patent WO2019107987A1, with IC50 values of 21 nM, 30 nM and 392 nM for C-RAF340D/Y341D, B-RAFV600E and B-RAFWT, 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.
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p38α inhibitor
p38α inhibitor 1 is a p38α inhibitor extracted from patent WO 2008076265 A1. -
MNK1 and MNK2 inhibitor
ETC-206 is a selective MNK1 and MNK2 inhibitor with IC50s of 64 nM and 86 nM, respectively. -
JNK inhibitor
CC-401 hydrochloride is a second generation ATP-competitive anthrapyrazolone c-Jun N terminal kinase (JNK) inhibitor with potential antineoplastic activity. -
Raf Inhibitor
CEP-32496 hydrochloride is a highly potent inhibitor of wild-type BRAF, V600E mutant BRAF and c-Raf with Kd values of 14 nM, 36 nM and 39 nM, respectively. -
MEK inhibitor
Cobimetinib R-enantiomer is the R-enantiomer of Cobimetinib, which is a potent, highly selective inhibitor of mitogen-activated protein kinase kinase(MEK1/2). -
Raf inhibitor
Dabrafenib Mesylate is a novel, potent, and selective Raf kinase inhibitor that is capableof inhibiting the kinase activity of wild-type B-Raf, B-RafV600Eand c-Raf with IC50 values of 3.2, 0.8, and 5.0 nM, respectively. -
Tyrosine kinase inhibitor
Regorafenib is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit, RET and Raf-1 with IC50 of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM, respectively. -
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. -
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. -
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. -
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 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.
