MAPK
Catalog No.
Product Name
Application
Product Information
Citations
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antioxidant agent
Ferulic acid methyl ester (Methyl Ferulate, Methyl 4'-hydroxy-3'-methoxycinnamate) is a lipophilic derivative of ferulic acid, which is a hydroxycinnamic acid that is abundant in plants. It shows the strongest antioxidant activity and can protect against inflammation and cancer. -
anti-inflammatory agent
Rotundic acid, a triterpenoid obtained from I. rotunda, induces DNA damage and cell apoptosis in hepatocellular carcinoma through AKT/mTOR and MAPK Pathways. Rotundic acid possesses anti-inflammatory and cardio-protective abilities. -
antithyroid agent
Methylthiouracil is an antithyroid agent. Methylthiouracil suppresses the production TNF-α and IL-6, and the activation of NF-κB and ERK1/2. -
antiinflammation agent
Ginsenoside Re (Ginsenoside B2) is an extract from Panax notoginseng. Ginsenoside Re decreases the β-amyloid protein (Aβ). Ginsenoside Re plays a role in antiinflammation through inhibition of JNK and NF-κB. - MMI-0100 is a cell-permeant peptide inhibitor of mitogen activated protein kinase activated protein kinase II (MK2). MMI-0100 reduces intimal hyperplasia ex vivo and in vivo. MMI-0100 suppresses IL-6 expression without effect on IL-8 expression. MMI-0100 suppresses fibrotic processes such as vein graft disease.
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JNK inhibitor
CC-90001 is a potent and selective JNK inhibitor. CC-90001 shows 12.9-fold selectivity for JNK1 over JNK2 in a cell-based model. CC-90001 can be used for the research of idiopathic pulmonary fibrosis -
raf kinase inhibitor
Raf inhibitor 2 is a potent raf kinase (IC50<1.0 μM) inhibitor, compound 32, extracted from patent EP1003721B1. Raf inhibitor 2 can be used for cancer research. -
TAK1 Inhibitor
5Z-7-Oxozeaenol is a selective and irreversible inhibitor of TAK1, exhibiting an IC50 of 8 nM. This compound also inhibits VEGF-R2 with an IC50 of 52 nM, demonstrating potential applications in anti-protozoan research and studies related to inflammation and tumorigenesis. Its unique mechanism of action makes it a valuable tool for exploring signaling pathways associated with cellular stress responses and vascular biology. -
PROTAC B-Raf Degrader
PROTAC B-Raf degrader 1 is a proteolysis targeting chimera (PROTAC) that facilitates the degradation of B-Raf through a Cereblon ligand. This compound demonstrates significant anti-cancer activity, making it a valuable tool for cancer research. It is particularly useful in studies investigating B-Raf-mediated signaling pathways and therapeutic strategies targeting oncogenic mutations in B-Raf. -
SOS1 Inhibitor
RMC-0331 is a potent and selective inhibitor of SOS1, designed for oral bioavailability. It effectively blocks RAS activation by disrupting the interaction between RAS and SOS1, making it a valuable tool compound for in vivo studies. This compound is suitable for exploring RAS signaling pathways and investigating therapeutic applications in cancer research. -
BRAFV600E Degrader
Tagarafdeg is a CRBN-based bifunctional degradation activating compound (BiDAC) selectively targeting BRAFV600E mutations. Demonstrating potent activity with a DC50 of 14 nM in A375 cells, it effectively degrades various BRAF mutations, including G469A and G466V, as well as the p61-BRAFV600E splice variant. This reagent is suitable for applications in tumor research, contributing to the understanding of BRAF-mediated oncogenic processes. -
MEK 1/2 Degrader
MS934 is a VHL-recruiting PROTAC degrader that targets MEK 1/2, facilitating their degradation alongside CRAF. This compound demonstrates significant biological activity in various cancer models, including melanoma, non-small cell lung cancer (NSCLC), colorectal cancer, primary brain tumors, and hepatocellular carcinoma. MS934 serves as an important tool for research into targeted cancer therapies and the mechanistic understanding of these oncogenic pathways. -
BRAF-V600E Degrader
PROTAC BRAF-V600E degrader-1 is an effective degrader of the BRAF-V600E mutant, selectively targeting this oncogenic variant while sparing wild-type BRAF. With Kd values of 2.4 nM and 2 nM for BRAF and BRAF-V600E, respectively, this compound facilitates degradation of BRAF-V600E through the ubiquitin-proteasome system (UPS). Its potent activity against melanoma cells makes it a valuable tool for research into targeted cancer therapies and mechanisms of drug resistance in BRAF-mutant tumors. -
RAF PROTAC Degrader
SJF-0628 is a RAF PROTAC degrader that facilitates the targeted degradation of BRAF protein in cancer cell lines, specifically in colorectal cancer models (Colo-205, LS-411N, HT-29, RKO) and the triple-negative breast cancer line DU-4475. This compound significantly reduces levels of phosphorylated MEK and ERK in DU-4475 cells, demonstrating notable anti-tumor activity. SJF-0628 is valuable for research studies focused on the mechanisms of colorectal cancer and triple-negative breast cancer. -
Endogenous Metabolite
Ergothioneine is an endogenous metabolite that acts as a potent antioxidant. It functions primarily as a specific inhibitor of p38 MAPK and Akt, which are critical signaling pathways involved in cellular stress responses. Ergothioneine is utilized in research focused on neuroprotection, cell apoptosis, and oxidative stress, making it a valuable compound for investigations into cellular resilience and health. -
SOS1 Inhibitor
SOS1-IN-14 is a potent and selective inhibitor of SOS1, demonstrating an IC50 value of 3.9 nM. This orally active compound is absorbed in the intestine through a P-glycoprotein-mediated efflux mechanism. SOS1-IN-14 is primarily utilized in research on KRAS-mutated cancers, showcasing superior tumor suppression capabilities compared to alternative therapies. -
SOS1/KRAS Inhibitor
SAH-SOS1A TFA is a peptide-based inhibitor targeting the SOS1-KRAS protein interaction. It exhibits nanomolar affinity for both wild-type and various mutant KRAS forms, including G12D, G12V, G12C, G12S, and Q61H (EC50 = 106-175 nM). By directly disrupting nucleotide association, SAH-SOS1A TFA effectively impairs KRAS-driven cancer cell viability and inhibits the downstream ERK-MAPK phosphosignaling cascade, making it a valuable tool for research in cancer biology. -
SOS1 Inhibitor
SOS1-IN-15 is a potent SOS1 inhibitor with an IC50 value of 5 nM, designed to specifically target and inhibit SOS1 activity. Its strong inhibitory effect makes it a promising candidate for research into KRAS-driven cancers, facilitating the understanding of oncogenic signaling pathways and development of targeted therapeutic strategies. -
Tyrosinase Inhibitor
Norartocarpetin is a potent tyrosinase inhibitor, demonstrating significant inhibition with an IC50 value of 0.47 μM. This compound serves as an effective antibrowning agent for food systems research and exhibits notable anticancer activity against lung carcinoma cells (NCI-H460) with an IC50 of 22 μM. Its antiproliferative effects are mediated through targeting the Ras/Raf/MAPK signaling pathway, inducing mitochondrial-mediated apoptosis, causing S-phase cell cycle arrest, and inhibiting cell migration and invasion in human lung carcinoma cells. -
Kinases PROTAC
DB1113 is a bifunctional compound designed for targeted protein degradation of various kinases. It effectively induces degradation of ABL1, ABL2, BLK, CDK4, CDK11B, EPHA3, MAPK7, RIPK1, and others, facilitating the investigation of kinase-related signaling pathways. DB1113 is suitable for research focusing on diseases or disorders associated with dysregulated kinase activity, providing a valuable tool for exploring therapeutic interventions in cancer and other conditions. -
CDK Inhibitor
Aloisine A is a potent cyclin-dependent kinase (CDK) inhibitor, exhibiting IC50 values of 0.15 μM for CDK1/cyclin B, 0.12 μM for CDK2/cyclin A, 0.4 μM for CDK2/cyclin E, and 0.16 μM for CDK5/p35. In addition to its CDK inhibitory effects, Aloisine A also inhibits GSK-3α and GSK-3β with IC50 values of 0.5 μM and 1.5 μM, respectively. Notably, it enhances the activity of wild-type and mutant CFTR with submicromolar affinity through a cAMP-independent mechanism, making it a valuable tool for research related to cystic fibrosis and CFTR-related disorders. -
Apoptosis Inducer
epi-Eriocalyxin A is a diterpenoid compound that serves as an apoptosis inducer in colon cancer cells. It effectively inhibits the activation of ERK1/2 and JNK pathways, leading to the suppression of Bcl-2 expression. This compound is valuable for research focused on cancer treatment and the mechanisms of apoptosis. -
Antiviral Agent
Dendrobine is an alkaloid derived from Dendrobium nobile, primarily targeting viral infections as an antiviral agent. It demonstrates significant antiviral activity against influenza A viruses, exhibiting IC50 values of 3.39 μM, 2.16 μM, and 5.32 μM for strains A/FM-1/1/47 (H1N1), A/Puerto Rico/8/34 H274Y (H1N1), and A/Aichi/2/68 (H3N2), respectively. Additionally, Dendrobine activates the JNK/p38/Nrf2 signaling pathway and possesses various biological properties, including antitumor, anti-inflammatory, and neuroprotective effects, making it valuable in diverse research applications. -
PPAR Activator
Bilobetin acts as a PPARα activator, enhancing lipid metabolism and insulin sensitivity. It effectively reduces blood lipid levels by promoting hepatic lipid uptake and oxidation, while decreasing triglyceride secretion and accumulation in tissues. Additionally, Bilobetin stimulates the phosphorylation and nuclear translocation of PPARα, resulting in increased cAMP levels and PKA activity. This compound is significant for research in metabolic disorders, particularly those related to insulin resistance and lipid regulation. -
Anticancer Agent
Citropten, also known as 5,7-dimethoxycoumarin, is a coumarin derivative with notable anticancer properties. It demonstrates significant anti-proliferative effects against A2058 and B16 melanoma cell lines, making it a valuable tool in cancer research. Additionally, Citropten exhibits anti-inflammatory activity by modulating the NFκB and MAPK signaling pathways. Its potential antidepressant effects are mediated through interactions with heat shock protein-70, monoamine oxidase-A, and the inhibition of apoptosis. -
MKK7-JNK Activator
MKK7-JNK Activator 1 is a potent activator of the MKK7-JNK signaling pathway. This compound effectively inhibits the proliferation and migration of MDA-MB-468 cells, while also triggering G2/M phase cell cycle arrest and caspase-dependent apoptosis, independent of reactive oxygen species (ROS) production. Notably, MKK7-JNK Activator 1 significantly increases the phosphorylation levels of MKK7 and JNK without affecting ERK or p38 phosphorylation. This reagent is valuable for studying mechanisms relevant to triple-negative breast cancer (TNBC). -
RAF-1/HIF-1α Inhibitor
MO-2097 is a selective RAF-1 and HIF-1α inhibitor that induces the destabilization of RAF-1, resulting in decreased levels of epithelial-mesenchymal transition (EMT) transcription factors and mesenchymal markers. Additionally, MO-2097 effectively inhibits HIF-1α protein expression mediated by hnRNPA2B1 in hypoxic conditions. This compound promotes the generation of mitochondrial reactive oxygen species (ROS), contributing to apoptosis in malignant cells. MO-2097 demonstrates significant potential in suppressing colorectal cancer metastasis by targeting the RAF/MEK/ERK signaling pathway and has shown efficacy in reducing tumor growth in HCT116 cell xenograft mouse models, thus serving as a valuable tool for colorectal cancer research. -
MEK/PI3K Inhibitor
ST-168 is an orally bioavailable inhibitor of MEK and PI3K, exhibiting IC50 values of 182 nM for MEK1 and showing varying potency against PI3K isoforms with values of 69.2 nM, 41.7 nM, 1482 nM, and 2293 nM for PI3Kα, PI3Kδ, PI3Kβ, and PI3Kγ, respectively. It effectively inhibits ERK1/2 and AKT phosphorylation, inducing apoptosis in cancer cells within a 3D tumor sphere model. In vivo studies demonstrate its substantial antitumor efficacy in A375 melanoma mouse models. Additionally, ST-168 displays an improved ocular safety profile compared to conventional MEK inhibitors, evidenced by reduced caspase activation and apoptosis levels, making it a valuable tool for melanoma research. -
SOS1 activator
VUBI1 (SOS1 Activator 1) is a benzimidazole-derived small molecule that acts as a potent activator of the guanine nucleotide exchange factor SOS1, with a dissociation constant (Kᴅ) of 44 nM. It promotes RAS activation by enhancing RAS-GTP formation and modulates downstream ERK phosphorylation, thereby influencing RAS–MAPK signaling. In addition, VUBI1 serves as a functional ligand for the development of PROTAC-based degraders, such as PROTAC SOS1 Degrader-1, to induce targeted SOS1 degradation. VUBI1 is a valuable compound for studying RAS pathway regulation and its role in cancer biology. -
SOS1 inhibitor
SOS1-IN-11 is a potent small-molecule inhibitor of SOS1, exhibiting an IC₅₀ value of 30 nM. It is used in research to disrupt the SOS1–KRAS interaction and modulate RAS signaling pathways in cancer models. - Pyridoxal 5′-phosphate monohydrate is the active coenzyme form of vitamin B6 and is essential for the function of numerous enzymes. It serves as a key cofactor for aromatic L-amino acid decarboxylase, which catalyzes the final step in the biosynthesis of the neurotransmitters dopamine and serotonin. Pyridoxal 5′-phosphate is the primary intracellular phosphorylated form of vitamin B6 and is interconvertible with other forms, including pyridoxine 5′-phosphate (PNP) and pyridoxamine 5′-phosphate (PMP).
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COX-2/MMP-7/TLR4 Inhibitor
Isofraxidin is a coumarin compound derived from *Acanthopanax senticosus* that exhibits anti-invasive and anti-inflammatory properties. It inhibits MMP-7 expression and suppresses cell invasion in human hepatoma cells by reducing ERK1/2 phosphorylation. Isofraxidin also downregulates the expression of iNOS and COX-2 and inhibits the formation of the TLR4/myeloid differentiation protein-2 (MD-2) complex. -
ERK2 inhibitor
Cafestol is an orally active diterpenoid and an inhibitor of ERK2. It exhibits multiple biological activities, including elevation of blood lipids, anti-inflammatory, anti-angiogenic, and anti-diabetic effects. Additionally, cafestol induces apoptosis and autophagy in tumor cells, making it a potential candidate for cancer research. - Lipoteichoic acid is an orally active compound with anti-inflammatory and antitumor properties. It is a key immune molecule found in Gram-positive bacteria that activates the complement system by upregulating C3 and inhibiting CD55. Lipoteichoic acid modulates macrophage autophagy via the PI3K/Akt/mTOR pathway, induces lung injury in mouse models, and inhibits melanin production.
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Kinases PROTAC/Nek9 Inhibitor
DB0614 is a PROTAC molecule utilizing a cereblon ligand, designed as a selective and potent degrader of NEK9 and other kinases. It induces the degradation of multiple kinases, including ABL1, ABL2, BLK, CDK11B, CDK4, CSK, EPHA3, FER, GAK, LIMK1, MAP3K20, MAP4K1–3, MAP4K5, MAPK14, MAPK7–9, MAPKAPK2/3, NLK, PDIK1L, PTK2B, RIPK1, RPS6KA1/3, SIK2/3, STK35, TNK2, and ULK1. DB0614 is suitable for research involving diseases or disorders driven by aberrant kinase activity. - Ganodermanontriol, a sterol isolated from *Ganoderma lucidum*, exerts anti-inflammatory effects in tert-butyl hydroperoxide (t-BHP)-damaged hepatic cells by upregulating heme oxygenase-1 (HO-1) expression. It demonstrates hepatoprotective activity.
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Gαq/11/14 Inhibitor
FR900359 is a cyclic depsipeptide and a selective inhibitor of Gαq/11/14 proteins in mammals. By targeting Gαq signaling, it effectively inhibits downstream pathways such as the ERK cascade. FR900359 has demonstrated the ability to suppress melanoma cell proliferation, lower blood pressure, and protect against airway hyperreactivity in murine models of allergen sensitization, such as the ovalbumin-induced asthma model. -
HPK1 inhibitor
NDI-101150 is an orally active, potent, and selective inhibitor of hematopoietic progenitor kinase 1 (HPK1). It enhances T cell activation and exhibits antitumor activity by promoting immune-mediated tumor suppression, making it a promising candidate for cancer immunotherapy research. -
PAF activator
C16-PAF (PAF (C16)) is a phospholipid mediator and a potent platelet-activating factor that functions as a ligand for the PAF G-protein-coupled receptor (PAFR). It exhibits anti-apoptotic effects by inhibiting caspase-dependent cell death through PAFR activation. C16-PAF is a strong activator of the MAPK and MEK/ERK signaling pathways and is known to induce increased vascular permeability. -
Erk Inhibitor
Edaxeterkib is a potent inhibitor of extracellular signal-regulated kinase (ERK), designed for cancer research. By targeting the ERK signaling pathway, Edaxeterkib interferes with tumor cell proliferation and survival, making it a valuable tool for studying ERK-driven malignancies. -
Osteoclast formation inhibitor
ABD56 is a bioactive compound that inhibits osteoclast formation and induces osteoclast apoptosis. Its mechanism of action involves suppression of the NFκB and ERK signaling pathways, making it a promising candidate for research in bone metabolism and osteolytic diseases. -
PPAR agonist
Lobeglitazone sulfate is a novel thiazolidinedione and an orally active agonist of peroxisome proliferator-activated receptors (PPARs), with EC50 values of 137.4 nM for PPARγ and 546.3 nM for PPARα. It also acts as an inhibitor of the ERK/JNK/Smad/NF-κB signaling pathways. Lobeglitazone sulfate exhibits anti-inflammatory, anti-diabetic, anti-fibrotic, and anti-atherosclerotic activities, supporting its potential in the treatment of metabolic and inflammatory diseases. - Hydrangenol is an orally active antiphotoaging compound isolated from *Hydrangea serrata* leaves. It prevents wrinkle formation by downregulating matrix metalloproteinases (MMPs) and inflammatory cytokines, while upregulating moisturizing factors and antioxidant gene expression, making it a promising agent for skin health and anti-aging research.
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ERK inhibitor
26-Deoxyactein, a bioactive constituent isolated from *Cimicifuga racemosa*, protects against TCDD-induced osteoblast damage. It exerts its effects by inhibiting the upregulation of aryl hydrocarbon receptor (AhR), CYP1A1, and ERK signaling, making it a potential agent for bone health and toxicology research.
