MAPK
Catalog No.
Product Name
Application
Product Information
Citations
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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. -
JNK Inhibitor
(3S)-Tanzisertib hydrochloride is a selective inhibitor of c-Jun N-terminal kinases (JNK), demonstrating IC50 values of 61, 7, and 6 nM for JNK1, JNK2, and JNK3, respectively. This compound also exhibits inhibition of ERK1, p38α, and EGFR with IC50 values of 0.48, 3.4, and 0.38 μM, respectively. (3S)-Tanzisertib hydrochloride effectively reduces LPS-induced TNFα production in an acute rat pharmacokinetic-pharmacodynamic model, making it a valuable tool in idiopathic pulmonary fibrosis research and other inflammatory disease studies. -
PI3K/Akt/Ras/Raf/MAPK Inhibitor
Erufosine is a potent inhibitor of the PI3K/Akt and Ras/Raf/MAPK signaling pathways. It demonstrates significant cytotoxic activity against breast cancer cell lines, specifically MCF-7 and MDA-MB-231, with IC50 values of 40.95 μM and 40.8 μM, respectively. By reducing the phosphorylation levels of PI3K (p85), Akt (PKB), and cRaf, Erufosine serves as a valuable tool in the research of breast cancer and myeloid leukemia. -
PI3K/AKT/BMP-2/p38/ERK 1/2 Modulator
Asperosaponin V is an indirect modulator of key signaling pathways, including PI3K/AKT, BMP-2/p38, and ERK 1/2. This compound stimulates the proliferation of marrow stromal cells and promotes differentiation into osteoblasts, making it valuable for studying bone metabolism. Asperosaponin V holds potential for applications in osteoporosis research and fracture healing studies. -
p38 MAPK Inhibitor
Licochalcone E is a flavonoid compound that functions as a p38 MAPK inhibitor. It effectively inhibits the transcriptional activities of NF-κB and AP-1 by disrupting AKT and MAPK activation pathways. This compound is valuable for research focused on inflammation, cancer, and signal transduction pathways, offering insights into cellular mechanisms influenced by MAPK signaling. -
ERK/Akt Activator
H-Ile-Lys-Val-Ala-Val-OH is a potent activator of the MAPK/ERK1/2 and PI3K/Akt signaling pathways. This compound enhances cell adhesion, promotes neurite outgrowth, and supports tumor growth. It is particularly effective in stimulating the proliferation of bone marrow-derived mesenchymal stem cells (BMMSCs), making it valuable for research applications in cell biology and regenerative medicine. -
p38 MAPK Inhibitor
AS1940477 is an orally active inhibitor of the p38 MAPK pathway, targeting both the p38α and p38β isoforms. It effectively reduces the production of pro-inflammatory cytokines, such as TNFα, IL-1β, and IL-6, in human synovial interstitial cells and relevant animal models of inflammation. This compound is a valuable tool for research aimed at understanding and treating inflammatory diseases. -
MAP4K4 Inhibitor
PF-06745013 is a selective inhibitor of MAP4K4, exhibiting an IC50 of 0.4 nM. This compound is distinguished by its lack of time-dependent inhibition risk for CYP3A4 and demonstrates non-ATP competitive activity. PF-06745013 has potential applications in the study of inflammatory diseases, including diabetes and cancer, making it a valuable tool in related research. -
p38α MAPK Inhibitor
rel-Talmapimod hydrochloride is a selective inhibitor of p38α MAPK, exhibiting an IC50 of 9 nM. By targeting the p38α MAPK pathway, rel-Talmapimod hydrochloride effectively inhibits the secretion of pro-inflammatory factors, including TNFα, IL-1β, IL-6, and VEGF, while also blocking angiogenesis and osteoclast activation. This compound has demonstrated the ability to inhibit the proliferation of multiple myeloma cells and induce apoptosis. It is suitable for research applications involving various hematological malignancies, such as multiple myeloma and myelodysplastic syndrome. -
p38 MAP Inhibitor
R-03201195 is a highly selective inhibitor of p38 MAP kinase, demonstrating an IC50 of 0.7 nM for p38α. It effectively inhibits TNF-α production in THP-1 cells and IL-1β in human whole blood, with IC50 values of 0.25 nM and 0.57 nM, respectively. This reagent is valuable for research applications in inflammatory diseases, particularly rheumatoid arthritis. -
RAF/DDR Inhibitor
PHI-501 is a dual inhibitor targeting RAF and DDR pathways. It demonstrates potent anti-proliferative effects in melanoma cell lines, effectively inhibiting colony formation in drug-resistant cells. PHI-501 disrupts ERK and AKT phosphorylation and downregulates key gene sets associated with TNFA-NFKB, IL6-JAK-STAT3, and KRAS signaling pathways, as well as pathways involved in epithelial-mesenchymal transition. In vivo studies show significant anti-tumor efficacy in the SK-MEL3DR xenograft model, making PHI-501 valuable for research on drug resistance in melanoma. -
p38α MAPK Inhibitor
BMS-751324 is a selective inhibitor of p38α MAPK, a key regulator in the inflammatory response pathway. This compound demonstrates significant anti-inflammatory effects, as evidenced by its ability to reduce foot swelling and inhibit LPS-induced TNFα production in an arthritic rat model. BMS-751324 is suitable for research applications focused on inflammation, arthritis, and related pathways. -
p38α Inhibitor
P38α-IN-10 is a selective inhibitor of p38α with an IC₅₀ of 230 nM. It effectively suppresses TNF production induced by lipopolysaccharide (LPS), making it a valuable tool for research into inflammatory responses. This compound is particularly relevant for studying conditions such as rheumatoid arthritis and septic shock, contributing to a deeper understanding of their underlying mechanisms. -
p38α MAPK Inhibitor
Talmapimod hydrochloride is a selective inhibitor of p38α MAPK, exhibiting an IC50 of 9 nM. This compound effectively suppresses the secretion of pro-inflammatory cytokines, including TNFα, IL-1β, IL-6, and VEGF, while also inhibiting angiogenesis and osteoclast activation. Talmapimod hydrochloride demonstrates efficacy in inhibiting the growth of multiple myeloma cells and promoting apoptosis, making it a valuable tool for investigating various hematological malignancies, such as multiple myeloma and myelodysplastic syndromes. -
ERK/BACE1/PSEN1 Inhibitor
L-Citronellol ((S)-3,7-Dimethyloct-6-en-1-ol) is an ERK/BACE1/PSEN1 inhibitor known for its anti-allergic and neuroprotective properties. This compound effectively inhibits mast cell activation and subsequent release of inflammatory mediators by targeting the ERK pathway. Additionally, L-Citronellol decreases the activity of BACE1, PSEN1, and acetylcholinesterase (AChE), while reducing TNF-α expression and lipid peroxidation, indicating its potential utility in multi-target approaches for Alzheimer's disease research. -
p38 MAPK Inhibitor
SR-318 is a selective inhibitor of p38 MAPK, exhibiting potent activity with IC50 values of 5 nM, 32 nM, and 6.11 µM for p38α, p38β, and p38α/β, respectively. This compound effectively reduces TNF-α release in whole blood, showing an IC50 of 283 nM. SR-318 is utilized in research focusing on anti-cancer and anti-inflammatory pathways, making it valuable for investigating therapeutic strategies in related diseases. -
p38 Inhibitor
TAT-MKK3b is a peptide inhibitor targeted at p38 mitogen-activated protein kinase (MAPK). It effectively inhibits p38 phosphorylation, contributing to its role in modulating cellular stress responses. TAT-MKK3b exhibits renal targeting, reactive oxygen species (ROS) scavenging, and the ability to mitigate ferroptosis. This compound has demonstrated potential in the improvement of acute kidney injury and may help prevent its progression to chronic kidney disease. -
MEK1/2 Inhibitor
RO5068760 is a potent non-ATP-competitive inhibitor of MEK1/2, demonstrating an IC50 of 0.025 μM for MEK1. This compound effectively inhibits MAPK pathway activity, leading to G1 cell cycle arrest and apoptosis, thereby reducing cancer cell proliferation. RO5068760 is applicable in research on various tumors characterized by dysregulation of the MAPK pathway, including melanoma, colorectal cancer, non-small cell lung cancer (NSCLC), and pancreatic cancer. -
JNK/c-Jun Activator
Ophiopogonin B primarily activates the JNK/c-Jun signaling pathway. This saponin compound, derived from Radix Ophiopogonjaponicus, demonstrates significant biological activity by inducing autophagy and apoptosis in colon cancer cells. It serves as a valuable reagent for researchers investigating mechanisms of cancer cell death and the therapeutic potential of autophagy modulation. -
JNK Inhibitor, ERK Inhibitor, TGFβ signaling Activator
(+)-Columbianetin targets JNK and ERK signaling pathways while acting as a TGFβ signaling activator. This compound effectively inhibits UVA-induced phosphorylation of JNK and ERK, decreases MMP-1 production, and reverses collagen degradation. In addition, it mitigates UVA-mediated suppression of Smad2/3 phosphorylation and translocation, providing protective effects against UV-induced cellular damage. (+)-Columbianetin is an essential tool for research focused on skin aging and oxidative stress responses in keratinocytes. -
Raf/EGFR Inhibitor
Lifirafenib maleate is a potent inhibitor of Raf kinase and EGFR, exhibiting IC50 values of 23 nM and 29 nM for recombinant BRafV600E and EGFR, respectively. This compound effectively disrupts critical signaling pathways involved in cancer cell proliferation and survival. Lifirafenib maleate is relevant for research applications in cancer biology, particularly in studies focusing on targeted therapies for tumors with BRAF mutations or EGFR dysregulation. -
EGFR/BRAF Inhibitor
EGFR/BRAF-IN-1 is a selective inhibitor targeting both EGFR and BRAFV600E with an IC50 of 45 nM. This compound, a 2,3-dihydropyrazino[1,2-a]indole-1,4-dione derivative, effectively inhibits cancer cell proliferation with a GI50 of 35 nM. Additionally, EGFR/BRAF-IN-1 exhibits notable antioxidant properties, making it a valuable reagent for research in cancer biology and therapeutic development. -
SOS1/EGFR Inhibitor
SOS1/EGFR-IN-1 is a dual-target inhibitor that specifically targets SOS1 and EGFR, demonstrating IC50 values of 42.13±1.55 nM and 1.01±0.04 nM, respectively. This compound effectively induces apoptosis and G1 phase cell cycle arrest, while reducing angiogenesis and cell migration. SOS1/EGFR-IN-1 exhibits significant antitumor activity in prostate cancer cells, with an IC50 of 0.45±0.03 μM, making it a valuable tool for research in cancer therapies. -
EGFR/ERK Activator
Astragaloside VI is an activator of the EGFR/ERK signaling pathway, primarily influencing cell proliferation and survival. It demonstrates significant biological activity in promoting wound healing processes through enhanced cellular responses. This compound serves as a valuable tool for research applications focused on tissue regeneration and repair mechanisms. -
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 Ihibitor
SB 202190 hydrochloride is a selective inhibitor of the p38 MAP kinase with IC50 values of 50 nM and 100 nM for p38α and p38β, respectively. By binding to the ATP pocket of active recombinant human p38 kinase with a Kd of 38 nM, it demonstrates significant anti-cancer activity. Furthermore, SB 202190 hydrochloride has been shown to induce autophagy, making it a valuable tool for research in cancer biology and signaling pathways related to stress response.
