MAPK
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Catalog No.
Product Name
Application
Product Information
Citations
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JNK inhibitor
JIP-1 (153-163) is a peptide inhibitor of c-Jun N-terminal kinase (JNK), based on residues 153-163 of JNK-interacting protein-1 (JIP-1). Binds to JNK with affinity in the micromolar range and minimally inhibits p38 and ERK. -
TOPK inhibitor
HI-TOPK-032 is a potent and selective TOPK inhibitor. In vitro, HI-TOPK-032 strongly suppressed TOPK kinase activity but had little effect on extracellular signal-regulated kinase 1 (ERK1), c-jun-NH2-kinase 1, or p38 kinase activities. -
JNK inhibitor
c-JUN peptide is a peptide comprising residues 33 - 57 of the JNK binding (δ) domain of human c-Jun. -
JNK inhibitor
TCS JNK 6o is a ATP-competitive and selective c-Jun N-terminal kinase (JNK) inhibitor. -
p38 MAPK inhibitor
DBM 1285 dihydrochloride is a p38 MAPK inhibitor. Supresses p38 phosphorylation and LPS-induced TNF-α production in macrophages and in vivo. -
JNK3 inhibitor
IQ-1S is a Selective JNK3 inhibitor with IC50 value of 390, 360 and 87 nM for JNK1, 2 and 3 respectively. -
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. -
raf kinase inhibitor
RAF709 is a potent inhibitor of B/C RAF kinase with almost equivalent IC50 values of 0.4 nM for B-RAF and C-RAF, showing a high level of selectivity, demonstrating greater than 99% on-target binding to BRAF, BRAFV600E, and CRAF at 1 μM and very few off-targets with DDR1 (>99%), DDR2 (86%), FRK (92%), and PDGFRb (96%), the only kinases with binding >80% at 1 μM. -
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. -
BRAF inhibitor
Lifirafenib (BGB-283), also known as Beigene-283, potently inhibits RAF family kinases and EGFR activities in biochemical assays with IC50 values of 23, 29 and 495 nM for the recombinant BRAFV600E kinase domain, EGFR and EGFR T790M/L858R mutant. -
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. -
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.
