MAPK
Catalog No.
Product Name
Application
Product Information
Citations
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B-RAF Inhibitor
ARQ-736 is a potent and selective inhibitor of the B-RAF kinase, which is integral to the MAPK signaling pathway. This compound demonstrates significant anticancer activity by selectively targeting B-RAF mutations commonly associated with various malignancies. ARQ-736 is valuable for research applications focused on understanding B-RAF-driven cancers and exploring targeted therapeutic strategies. -
MEK1/C-Raf Inhibitor
MEK1/C-Raf-IN-1 is a selective inhibitor of MEK1 and C-Raf, exhibiting IC50 values of 97 nM and 23 nM, respectively. This compound demonstrates significant antitumor activity, making it a valuable tool for research in cancer biology and therapeutic development. Its effects on MAPK signaling pathways provide insights into potential treatment mechanisms for various malignancies. -
RAF Inhibitor
RAF-IN-2 is a selective RAF inhibitor that disrupts RAF-MEK-ERK signaling pathways. This compound demonstrates significant activity against various proliferative diseases, including leukemia, psoriasis, and fibrosis. Its application in research facilitates investigations into the mechanisms of these diseases and the potential therapeutic benefits of targeted RAF inhibition. -
B-RafV600E Inhibitor
EBI-907 is a potent and orally active inhibitor of the B-RafV600E mutation. It exhibits significant antiproliferative activity in cancer cell lines, demonstrating IC50 values of 13 nM in A375 and 14 nM in Colo-205 cells. In vivo studies show that EBI-907 effectively induces tumor regression in a Colo-205 xenograft model dependent on B-RafV600E. This compound is a valuable tool for research focused on melanoma and cancers associated with B-RafV600E mutations. -
BRAF V600E/CRAF Inhibitor
BRAF V600E/CRAF-IN-2 is a potent inhibitor targeting BRAF V600E and CRAF, demonstrating IC50 values of 0.888 μM and 0.229 μM, respectively. This compound induces apoptosis and effectively causes cell cycle arrest at the G0/G1 phase in HCT-116 colon cancer cells. BRAF V600E/CRAF-IN-2 is suitable for research applications focused on cancer biology and treatment strategies. -
B-Raf Inhibitor
B-Raf IN 6 is a highly potent inhibitor of the B-Raf protein kinase, exhibiting an IC50 of 1.7 nM. This compound selectively targets B-Raf without significant binding to the secondary target PXR and demonstrates resistance to rapid metabolism. B-Raf IN 6 is valuable for research applications focusing on cancer biology and therapeutic development. -
BRAF V600E/CRAF Inhibitor
BRAF V600E/CRAF-IN-1 (Compound 8b) is a potent inhibitor targeting BRAF V600E and CRAF. It induces apoptosis and effectively causes cell cycle arrest at the G0/G1 phase in HCT-116 colon cancer cells. This compound is valuable for research into cancer pathophysiology and therapeutic interventions. -
b/cRAF Inhibitor
RAF-IN-1 is a potent inhibitor of b/cRAF, demonstrating IC50 values of 3.8 nM for cRAF, 36 nM for bRAF wild-type, and 29.4 nM for the bRAFV600E mutant. This compound effectively inhibits cell growth in cancer cell lines harboring the bRAFV600E mutation, with GI50 values of 3.4 nM in H358 and 2.9 nM in A375 cells. RAF-IN-1 is valuable for research in cancer biology, particularly in studies targeting the RAS-RAF-MEK-ERK signaling pathway. -
BRAF Inhibitor
B-Raf IN 14 is a selective inhibitor of the BRAF kinase, exhibiting an IC50 value of 11.08 μM. This compound is valuable in cancer research, particularly in studies investigating BRAF mutations and their role in tumor progression. Its application may extend to evaluating the efficacy of targeted therapies in BRAF-driven malignancies. -
PROTAC BRAF-V600E Degrader
PROTAC BRAF-V600E Degrader-2 is a highly selective degrader targeting the BRAF-V600E mutant, with dissociation constants (Kd) of 14.4 nM and 9.5 nM for BRAF and BRAF-V600E, respectively. This compound effectively induces degradation of the BRAF-V600E kinase domain without impacting wild-type BRAF. Its potent biological activity makes it a valuable tool for research applications focused on melanoma cell growth inhibition and the study of BRAF-related signaling pathways. -
B-Raf Inhibitor
B-Raf IN 8 is a potent inhibitor of the B-Raf kinase, exhibiting an IC50 of 70.65 nM. This compound demonstrates significant antitumor activity across various cancer cell lines, including hepatocellular carcinoma (HEPG-2), colon carcinoma (HCT-116), mammary gland cancer (MCF-7), and human prostate cancer (PC-3), with IC50 values of 9.78 µM, 13.78 µM, 18.52 µM, and 29.85 µM, respectively. B-Raf IN 8 is a valuable tool for research into targeted cancer therapies and the mechanistic pathways associated with B-Raf signaling. -
BRAF Inhibitor
Everafenib is a highly selective BRAF inhibitor that effectively penetrates the blood-brain barrier (BBB) and inhibits MAPK signaling pathways. It demonstrates potent activity against various V600E BRAF melanoma cell lines, with IC50 values ranging from 2 to 10 nM, showcasing superior potency compared to other BRAF inhibitors. In vitro and in vivo studies indicate its efficacy in treating metastatic melanoma, including significant effects observed in an intracranial mouse model. This makes Everafenib a valuable tool for cancer research and therapeutic developments targeting BRAF mutations. -
BRAF Inhibitor
B-Raf IN 19 is a specific BRAF inhibitor targeting both BRAF wild-type (BRAF WT) and BRAF V600E mutants, with IC50 values of 0.57 μM and 0.28 μM, respectively. This compound effectively disrupts MAPK signaling pathways in melanoma cells, making it a valuable tool for research focused on cancer signaling mechanisms and therapeutic interventions in melanoma. Its selective inhibition profile supports its use in studies aimed at understanding BRAF-related oncogenic processes. -
Raf Inhibitor
Raf Inhibitor 3 specifically targets Raf kinases, including B-Raf and C-Raf, with IC50 values below 15 nM. This compound demonstrates potent inhibitory activity, making it a valuable tool for research focused on oncogenic signaling pathways in cancer. Raf Inhibitor 3 is suitable for studying the role of Raf kinases in tumor biology and evaluating potential therapeutic strategies against Raf-dependent malignancies. -
BRAF Inhibitor
B-Raf IN 16 is a selective BRAF inhibitor designed to target the BRAF protein, a key regulator in the MAPK signaling pathway. This cyclic iminopyrimidine derivative exhibits potent anti-cancer activity by impeding the proliferation of BRAF-mutant tumor cells. B-Raf IN 16 is primarily applied in cancer research, aiding in the exploration of targeted therapies for BRAF-related malignancies. -
B-Raf Inhibitor
B-Raf IN 18 is a potent B-Raf inhibitor with an IC50 of 3.8 nM. It effectively targets the B-Raf protein, playing a critical role in the MAPK/ERK signaling pathway, which is often dysregulated in various cancers. This compound is suitable for anti-cancer research applications, providing a valuable tool for investigating B-Raf’s involvement in tumor progression and potential therapeutic strategies. -
RAF Inhibitor
XL-281 is a potent and selective inhibitor of RAF kinase, demonstrating IC50 values of 2.6 nM for CRAF, 4.5 nM for B-RAF, and 6 nM for B-RAFV600E. This compound exhibits significant antitumor activity, making it a valuable tool for cancer research. It is particularly relevant for studies targeting RAF signaling pathways in various malignancies. -
Raf Kinase Inhibitor
RAF-IN-4 is a potent Raf Kinase inhibitor, demonstrating IC50 values of 134.3 nM for B-Raf, 118.6 nM for B-Raf (V600E), and 276.7 nM for C-Raf. This compound effectively inhibits the proliferation of cancer cells by targeting the Raf signaling pathway, making it a valuable tool for research in cancer biology, particularly in lung and breast cancer studies. Its selective inhibition of Raf Kinases allows for detailed exploration of their role in oncogenesis and potential therapeutic interventions. -
RAF Inhibitor
IHMT-RAF-128 is a highly potent pan-RAF inhibitor targeting the RAF kinase family, which plays a crucial role in cell signaling and oncogenesis. This compound exhibits significant antitumor efficacy in xenograft mouse models, demonstrating its potential as a therapeutic agent in cancer research. Notably, IHMT-RAF-128 shows minimal toxicity, making it an attractive candidate for further investigation in oncological studies. -
Ligand of BRAF
BRAF ligand-1 acts as a specific ligand for the BRAF protein, playing a crucial role in the regulation of cell signaling pathways associated with cell proliferation, survival, and differentiation. This compound is important for studying the BRAF signaling pathway and its implications in various cancers. Additionally, BRAF ligand-1 can be utilized in the synthesis of CST905, further enhancing its utility in biochemical research and drug discovery efforts targeting mutant BRAF. -
p38 MAPK Inhibitor
Gossypetin is a hexahydroxylated flavonoid that primarily targets the p38 MAPK signaling pathway by inhibiting mitogen-activated protein kinase kinases MKK3 and MKK6. This inhibition effectively attenuates the MKK3/6-p38 signaling pathway, leading to multiple pharmacological effects, including antioxidant, antibacterial, and anticancer activities. Gossypetin is of interest in research exploring therapeutic applications against various diseases mediated by p38 MAPK signaling dysregulation. -
p38 Inhibitor
N-Acetylmuramic acid is a key component of the bacterial cell wall peptidoglycan, targeting the p38 MAPK signaling pathway. It plays a critical role in maintaining cell shape and integrity in bacterial species, particularly Bacteroides forsythus, while also inhibiting spore germination through the inhibition of hexosaminidase and core enzymes. Additionally, N-acetylmuramic acid exhibits significant anti-inflammatory activity, making it a valuable reagent in studies of cellular proliferation and inflammatory responses. This compound is noted for its oral bioactivity. -
NF-κB p65 Inhibitor, p38 MAPK Inhibitor
PSMα3 is an inhibitor of NF-κB p65 and p38 MAPK, playing a significant role in modulating inflammatory pathways. This compound forms membrane pores and interacts with the human insulin B chain, inhibiting insulin aggregation and contributing to cytotoxic effects through α-type amyloid-like fibril formation. PSMα3 is valuable for research on spondyloarthritis, rheumatoid arthritis, insulin-derived amyloidosis, and infections caused by Staphylococcus aureus. -
p38 MAPK Inhibitor
Bisabolangelone is a potent inhibitor of the p38 MAPK pathway. Isolated from the roots of Osterici Radix, this sesquiterpene derivative demonstrates significant anti-inflammatory activity by inhibiting LPS-stimulated inflammation through the blockade of the NF-kappaB and MAPK signaling pathways in macrophages. Additionally, Bisabolangelone exhibits anti-ulcer activities, making it a valuable tool in studies related to inflammation and gastrointestinal disorders. -
p38 MAPK Inhibitor
p38 MAP Kinase Inhibitor III is a potent inhibitor of p38 MAPK, with an IC50 value of 0.9 μM. This compound also effectively reduces the release of pro-inflammatory cytokines, specifically IL-1β and TNF-α, with IC50 values of 0.37 μM and 0.044 μM, respectively. p38 MAP Kinase Inhibitor III is valuable for research in inflammation, signaling pathways, and related therapeutic applications. -
p38α Inhibitor
Emprumapimod is a selective inhibitor of p38α MAPK that exhibits potent oral activity. By directly inhibiting LPS-induced IL-6 production in RPMI-8226 cells (IC50=100 pM), it presents significant anti-inflammatory properties. This compound is applicable in research studies focused on dilated cardiomyopathy and acute inflammatory pain, making it a valuable tool for elucidating the role of p38α in various inflammatory conditions. -
MEK1 Inhibitor
Nedometinib is a selective MEK1 inhibitor, demonstrating an IC50 of 135 nM. By inhibiting phosphorylated ERK (p-ERK) in the MAPK signaling pathway, Nedometinib exhibits notable anticancer activity against squamous cell carcinoma. This compound is valuable for research applications related to dermatosis and neurofibromatosis. -
TAK1-MKK3 PPI Inhibitor
(R)-STU104 is a selective inhibitor of the TAK1-MKK3 protein-protein interaction, demonstrating potent activity with IC50 values of 0.58 μM for TNF-α and 4.0 μM for MKK3 phosphorylation. By binding to MKK3, (R)-STU104 effectively disrupts the TAK1-mediated phosphorylation of MKK3, subsequently inhibiting the TAK1/MKK3/p38/MnK1/MK2/eIF4E signaling pathway. This compound is a valuable tool for investigating the molecular mechanisms underlying ulcerative colitis and related inflammatory conditions. -
p38α MAPK Inhibitor
p38α Inhibitor 2 is a highly selective inhibitor of the p38α mitogen-activated protein kinase (MAPK), exhibiting a pIC50 value of 9.6. This compound demonstrates potent inhibition of the hERG ion channel with an IC50 of 27 μM. Additionally, p38α Inhibitor 2 shows an excellent selectivity profile, demonstrating less than 30% inhibition across a panel of 51 protein kinases at a concentration of 10 μM, indicating its potential utility in various biological research applications focused on inflammation and stress responses. -
p38α Inhibitor
SD-169 is an orally active ATP-competitive inhibitor of p38α MAPK, exhibiting an IC50 of 3.2 nM. This compound also demonstrates weak inhibition of p38β MAPK with an IC50 of 122 nM. SD-169 has been shown to impede the development and progression of diabetes by inhibiting T cell infiltration and activation, making it valuable for research in immunology and metabolic disease pathways. -
p38 MAPK Inhibitor
p38 MAPK-IN-4 is a selective inhibitor of p38 mitogen-activated protein kinase (MAPK) with an IC50 of 35 nM. This compound modulates the p38 MAPK signaling pathway, which is critical in cellular responses to stress and inflammation. It is suitable for research applications investigating inflammatory diseases, cancer, and other conditions associated with p38 MAPK activity. -
Anti-inflammatory/Anti-fibrotic Agent
GDC-3280 is an orally active anti-inflammatory and anti-fibrotic agent that operates primarily through the inhibition of the ASK1-p38 MAPK pathway. It effectively mitigates the inflammatory and fibrotic responses associated with silicosis and influences macrophage polarization. GDC-3280 is a valuable tool for research aimed at understanding and developing therapeutic strategies for inflammatory and fibrotic diseases. -
p38α MAPK Inhibitor
p38 MAP Kinase Inhibitor IV is a selective ATP-competitive inhibitor targeting p38α MAPK, exhibiting IC50 values of 0.13 μM and 0.55 μM for p38α and p38β MAPK, respectively. This compound plays a crucial role in modulating cellular responses to stress and inflammation by inhibiting the p38 MAPK signaling pathway. It is utilized in research applications focused on therapeutic interventions for inflammatory diseases and various cancer models. -
p38 MAPK Inhibitor, coumarin, glucoside
Esculin sesquihydrate is a coumarin glucoside that serves as an inhibitor of p38 MAPK. This compound has demonstrated significant biological activity in ameliorating cognitive impairment associated with experimental diabetic nephropathy. Additionally, esculin sesquihydrate exhibits antioxidant and anti-inflammatory properties, primarily through modulation of the MAPK signaling pathway, making it valuable for research in diabetes-related complications and inflammation studies. -
p38α/β Degrader
NR-7h is a selective degrader of p38α and p38β, exhibiting DC50 values of 24 nM and 27.2 nM for p38α in T47D and MB-MDA-231 cells, respectively. This compound effectively induces degradation of these kinases, facilitating the study of their roles in cellular signaling pathways. NR-7h is applicable in cancer research and other studies investigating inflammatory responses and signal transduction mechanisms. -
p38 MAPK Inhibitor
PF-03715455 is a selective p38 MAPK inhibitor with significant potency, demonstrating IC50 values of 0.88 nM for p38α and 23 nM for p38β. This compound effectively inhibits LPS-induced TNFα production in human whole blood, with an IC50 of 1.7 nM. PF-03715455 has potential applications in research focusing on chronic obstructive pulmonary disease (COPD) and inflammation-related pathways. -
DDR/p38 Inhibitor
SR-302 is a selective DDR/p38 inhibitor that exhibits potent biological activity with IC50 values of 0.125 μM for p38α, 0.023 μM for DDR1, and 0.018 μM for DDR2. This compound is valuable for investigating fibrotic disorders, including renal and pulmonary fibrosis, atherosclerosis, and various types of cancer. SR-302 serves as a key tool for elucidating the roles of DDR and p38 signaling pathways in disease progression and therapeutic intervention. -
p38/MAPK Inhibitor
LX-3 is a selective inhibitor of the p38 MAPK signaling pathway. It effectively modulates gene expression by reactivating silenced EGFP reporter genes associated with DNA methylation, including TNF, EGR1, LY6K, and ISG20. This reagent is valuable for studies investigating the roles of p38 MAPK in cellular processes and the impact of DNA methylation on gene regulation. -
p38 Inhibitor
p38α inhibitor 5 is a PROTAC-type ligand that specifically targets p38α MAP kinase. This compound is designed to facilitate the degradation of p38α, providing a valuable tool for studying the enzyme's role in cellular signaling and inflammation. It is suitable for applications in drug discovery and therapeutic research, particularly in the context of conditions associated with p38α dysregulation. -
p38 Inhibitor
Org 48762-0 is a selective p38 inhibitor, exhibiting a potent EC50 of 0.1 μM for p38α kinase. This compound demonstrates a high degree of specificity for both p38α and p38β over other kinases, allowing for targeted therapeutic interventions. Org 48762-0 effectively reduces lipopolysaccharide-induced TNFα release, making it a valuable tool in the study of inflammatory diseases. Its applications extend to researching conditions such as rheumatoid arthritis and Werner syndrome. -
p38α Inhibitor
Cyclocurcumin is a potent inhibitor of p38α, a key signaling molecule involved in inflammatory responses. It demonstrates significant antirheumatic, antivasoconstrictive, and antioxidant activities. This compound is valuable for research applications focused on inflammation, cardiovascular diseases, and oxidative stress. -
TAK1/p38α Inhibitor
PF-05381941 is a potent dual inhibitor of TAK1 and p38α, exhibiting IC50 values of 156 nM and 186 nM, respectively. This compound effectively modulates the MAPK signaling pathway, making it a valuable tool for investigating cellular responses to stress and inflammation. PF-05381941 is commonly utilized in research focused on cancer, autoimmune diseases, and other pathological conditions linked to dysregulated kinase activity. -
p38 MAPK Inhibitor
RO3201195 is a selective inhibitor of p38 MAPK, a key signaling molecule involved in inflammatory responses and cellular stress. This compound demonstrates potent inhibition of WS cell proliferation, with an IC50 value of 190 nM. RO3201195 is suitable for research applications aimed at understanding the role of p38 MAPK in various biological processes, including inflammation and cancer. -
MEK Inhibitor
Zapnometinib is a potent MEK inhibitor with an IC50 of 5.7 nM, acting primarily on the MAPK/ERK signaling pathway. This compound displays antiviral activity against the influenza virus and possesses antibacterial properties, making it a valuable tool for research applications in virology and microbiology. Its efficacy in inhibiting MEK highlights its potential for studies related to cancer and inflammatory diseases. -
MEK Inhibitor
MEK-IN-9 is a selective inhibitor of the MEK (mitogen-extracellular signal-regulated kinase) pathway. This compound has been shown to induce the expression of the tumor suppressor proteins p15 and p27, contributing to its anti-proliferative effects. MEK-IN-9 is suitable for research focusing on renal adenocarcinoma and colorectal cancer, making it a valuable tool for studying the mechanisms of tumor growth and potential therapeutic interventions. -
Raf/MEK/MAPK Pathway Inhibitor
2-Bromoaldisine is a pyrrole alkaloid that acts as a potent inhibitor of the Raf/MEK/MAPK signaling pathway. It is known to effectively suppress HIV-1 vector infection. This compound is valuable for research applications focused on cancer biology and viral pathogenesis, allowing investigators to study the effects of Raf/MEK/MAPK pathway modulation on cell proliferation and viral replication. -
MEK/PI3K Inhibitor
MEK/PI3K-IN-2 is a potent inhibitor targeting both MEK and PI3K pathways, exhibiting IC50 values of 352 nM for MEK1, 107 nM for PI3Kα, and 137 nM for PI3Kδ. This compound effectively reduces levels of phosphorylated AKT and ERK1/2, demonstrating significant anti-proliferative activity against various tumor cell lines. MEK/PI3K-IN-2 is valuable for research in cancer biology and therapeutic development aimed at disrupting these critical signaling pathways. -
SOS1 Inhibitor
SOS1-IN-22 is a selective inhibitor of the son of sevenless homolog 1 (SOS1), crucial for the formation of the KRAS-G12C/SOS1 complex with an IC50 value of 40.28 nM. This compound effectively reduces ERK phosphorylation levels, influencing downstream signaling pathways. SOS1-IN-22 is intended for research applications in cancer biology, particularly relevant to pancreatic carcinoma and appendiceal carcinoma. -
MEK/PI3K Inhibitor
MEK/PI3K-IN-1 is a potent inhibitor targeting MEK and PI3K pathways, exhibiting IC50 values of 124 nM for MEK1, 130 nM for PI3Kα, and 236 nM for PI3Kδ. This compound effectively reduces levels of phosphorylated AKT (pAKT) and ERK1/2 (pERK1/2), demonstrating significant anti-proliferative effects in various tumor cell lines. MEK/PI3K-IN-1 serves as a valuable tool for research in cancer therapeutics and signaling pathway analysis. -
HPK1 Inhibitor
HPK1-IN-69 is a potent inhibitor of HPK1 with an IC50 of 1.7 nM. This compound disrupts the HPK1-mediated T cell receptor signaling pathway, decreasing SLP76 phosphorylation and enhancing IL-2 release. In vivo studies demonstrate its anti-tumor efficacy in mouse models, making it a valuable reagent for investigating colorectal cancer and MC38 syngeneic tumors.
