MAPK
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Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
fMLP inhibitor
Larixol is an fMLP inhibitor that also suppresses key signaling pathways involved in immune regulation, including Src kinase, ERK1/2, p38, and AKT phosphorylation. It disrupts the interaction between the βγ subunit of the fMLP receptor Gi protein and downstream effectors, thereby inhibiting fMLP-induced respiratory burst. Larixol effectively inhibits fMLP (0.1 μM)-induced superoxide anion production (IC50: 1.98 μM), cathepsin G release (IC50: 2.76 μM), and neutrophil chemotaxis. It mitigates neutrophil hyperactivation and helps reduce inflammation and tissue damage. Additionally, Larixol derivatives have shown inhibitory activity against TRPC6 functional mutants associated with focal segmental glomerulosclerosis (FSGS). -
ERK1/2 inhibitor
SHR2415 is a highly potent, selective, and orally active ERK1/2 inhibitor with IC50 values of 2.8 nM for ERK1 and 5.9 nM for ERK2. It demonstrates strong antiproliferative activity in Colo205 cells with an IC50 of 44.6 nM. SHR2415 is a promising compound for cancer research, particularly in targeting the MAPK/ERK signaling pathway. -
LSF inhibitor
FQI1 is a selective inhibitor of Late SV40 Factor (LSF), a transcription factor implicated in oncogenesis. It suppresses cell proliferation with IC50 values of 3 μM in NIH/3T3 cells, 0.79 μM in HeLa cells, and 6.3 μM in A549 cells. FQI1 is a valuable tool for cancer research targeting LSF-driven pathways. -
SOS1 inhibitor
RGT-018 is a potent, orally active SOS1 inhibitor that exhibits anti-tumor activity by blocking KRAS activation. By disrupting the SOS1–KRAS interaction, RGT-018 effectively inhibits cancer cell proliferation, making it a promising candidate for targeting KRAS-driven malignancies. -
MEK1/2 inhibitor
Tunlametinib is a highly selective, orally active MEK1/2 inhibitor with an IC50 of 1.9 nM against MEK1. It effectively blocks the RAS-RAF-MEK-ERK signaling cascade, inducing cell cycle arrest and apoptosis. Tunlametinib exhibits strong antiproliferative activity against RAS/RAF mutant cancer cells, including BRAF^V600E and KRAS^G12C mutants, and shows synergistic anti-tumor effects when combined with BRAF, KRAS^G12C, or SHP2 inhibitors, as well as Docetaxel. It is a promising agent for the study of targeted therapies in RAS/RAF-driven malignancies such as melanoma, colorectal cancer, and non-small cell lung cancer. -
HPK1/MAP4K1 inhibitor
PF-07265028 is a selective inhibitor of hematopoietic progenitor kinase 1 (HPK1/MAP4K1) with potent cellular activity, demonstrated by a pSLP76 IC50 of 17 nM. It is a promising compound for cancer research, particularly in studies involving immune regulation and tumor immunotherapy. -
SHP2 inhibitor
Migoprotafib (GDC-1971; compound 199) is a selective SHP2 inhibitor that suppresses the MAPK/ERK signaling pathway. It exhibits antitumor activity and is under investigation for its potential in targeting SHP2-driven cancers. -
PGAM1 inhibitor
HKB99 is an allosteric inhibitor of phosphoglycerate mutase 1 (PGAM1) that induces apoptosis and suppresses cell migration by inhibiting the formation of invasive pseudopodia. It increases oxidative stress, activates the JNK/c-Jun pathway, and downregulates AKT and ERK signaling. HKB99 is a promising compound for the study of non-small cell lung cancer (NSCLC). -
ALK/ROS1 inhibitor
Iruplinalkib (WX-0593) is an orally active and selective ALK/ROS1 inhibitor that effectively blocks tyrosine autophosphorylation of ALK, mutant ALK, and EGFR, with IC50 values ranging from 5.38 to 16.74 nM. Additionally, it inhibits the transport activity of MATE1, MATE2K, P-gp, and BCRP. Iruplinalkib is under investigation for the treatment of non-small cell lung cancer (NSCLC). -
Endoplasmic Reticulum Stress Inhibitor
Tauroursodeoxycholate (Tauroursodeoxycholic acid; TDUCA) dihydrate is an inhibitor of endoplasmic reticulum (ER) stress that significantly downregulates pro-apoptotic molecules, including caspase-3 and caspase-12. Additionally, it suppresses ERK signaling, contributing to its cytoprotective and anti-apoptotic effects. -
MEK1/2 inhibitor
MAP855 is a highly potent, selective, ATP-competitive, and orally active MEK1/2 kinase inhibitor, with an IC50 of 3 nM for the MEK1–ERK2 cascade and a pERK EC50 of 5 nM. It exhibits equipotent inhibitory activity against both wild-type and mutant forms of MEK1/2, making it a valuable tool for MAPK pathway research. -
PDGFR Inhibitor
Methylnissolin (Astrapterocarpan), a natural compound isolated from *Astragalus membranaceus*, inhibits PDGF-BB-induced vascular smooth muscle cell proliferation with an IC50 of 10 μM. It exerts its effects by suppressing PDGF-BB-induced phosphorylation of ERK1/2, thereby blocking activation of the ERK1/2 MAP kinase signaling cascade. -
ADAM17 inhibitor
JG26 is a potent ADAM inhibitor with IC50 values of 12 nM for ADAM8, 1.9 nM for ADAM17, and 150 nM for ADAM10. It also inhibits MMP-12 with an IC50 of 9.4 nM. JG26 suppresses AngII-induced EGFR transactivation and ERK activation, upregulates ACE2 expression, inhibits CD23 shedding, and reduces SARS-CoV-2 infection. Additionally, JG26 demonstrates anti-metastatic effects in colorectal cancer and holds research potential in Hodgkin lymphoma and vascular diseases. -
CK2/ERK8 inhibitor
TMCB (CK2/ERK8-IN-1) is a dual inhibitor of casein kinase 2 (CK2) and ERK8 (MAPK15/ERK7), with a Ki of 0.25 µM for CK2 and IC50 values of 0.50 µM for both targets. It also exhibits binding affinity for PIM1 (Ki = 8.65 µM), HIPK2 (Ki = 15.25 µM), and DYRK1A (Ki = 11.9 µM). CK2/ERK8-IN-1 demonstrates pro-apoptotic activity and is a useful tool for studying kinase-mediated cell survival pathways. -
NF-κB inhibitor
Asperulosidic Acid (ASPA) is a bioactive iridoid glycoside isolated from the herb Hedyotis diffusa Willd., exhibiting anti-tumor, antioxidant, and anti-inflammatory properties. Its anti-inflammatory effects are associated with the downregulation of proinflammatory cytokines such as TNF-α and IL-6, mediated through inhibition of the NF-κB and MAPK signaling pathways. -
ERK1/2 inhibitor
ASN007 (ERK-IN-3) benzenesulfonate is a potent, orally active ERK1/2 inhibitor with low single-digit nanomolar IC50 values. It is under investigation for the treatment of cancers driven by RAS mutations. -
ERK1/2 Inhibitor
ERK1/2 Inhibitor 7 is a highly potent ERK inhibitor, exhibiting an IC50 of 0.94 nM against ERK2. It is referenced in patent WO2021110168A1 (compound WX006). -
VEGFR-3 inhibitor
EVT801 is an orally active, selective VEGFR-3 inhibitor (IC50=11 nM) with potent antitumor properties. It suppresses VEGF-C-induced human endothelial cell proliferation and tumor-associated lymphatic angiogenesis in mouse models. EVT801 reduces tumor hypoxia, immunosuppressive cytokines (CCL4, CCL5), and myeloid-derived suppressor cell (MDSC) production. When combined with immune checkpoint therapy (ICT), EVT801 enhances response rates and improves tumor inhibition in cancer mouse models. Additionally, EVT801 is a click chemistry reagent containing an alkyne group, enabling copper-catalyzed azide-alkyne cycloaddition (CuAAC) with azide-containing molecules.
