MAPK
Catalog No.
Product Name
Application
Product Information
Citations
-
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. -
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 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. -
MEK1/2 inhibitor
AS703026 is a novel, selective, orally bioavailable MEK1/2 inhibitor that inhibits growth and survival of MM cells and cytokine-induced osteoclast differentiation. -
p38 MAPK inhibitor
LY2228820 is a novel and potent p38MAPK inhibitor with potent antiinflammatory activity. -
RAF/VEGFR Inhibitor
RAF265 (CHIR-265) is an oral, highly selective RAF and VEGFR kinase inhibitor, which is to control or normalize VEGFR-2 along with the inhibition of B-raf and c-Raf mutation to prevent cancers. -
RAF/VEGFR Inhibitor
Raf265 derivative is a derivative of Raf265 that is an oral, highly selective RAF and VEGFR kinase inhibitor with IC50 of of 5 to 10 μM. -
p38 MAPK inhibitor
Pexmetinib is a potent inhibitor of cytokine synthesis, via the dual inhibition of p38 mitogen-activated protein kinase (MAPK), and Tie2/Tek receptor tyrosine kinase. -
p38 MAPK inhibitor
VX-745 is a small-molecule inhibitor of MAPK that is reported to be active against several isotypes of p38 MAPK, including p38α, p38βand p38γ . -
p38 MAPK inhibitor
SKF 86002 Dihydrochloride is inhibitor of p38 MAP kinase (IC50 = 0.1 - 1 uM). Potently inhibits LPS-induced IL-1 and TNF-α production in human monocytes (IC50 = 1 uM). -
p38 MAPK inhibitor
SB 203580 hydrochloride (Adezmapimod hydrochloride) (RWJ 64809 hydrochloride) is a widely used p38 MAPK inhibitor.
-
MAPKAPK2(MK2) inhibitor
MK2-IN-1 hydrochloride is a potent and selecitve MAPKAPK2(MK2) inhibitor(IC50=0.11 uM) with a non-ATP competitive binding mode. -
ALK/MET inhibitor
Ensartinib hydrochloride (X-396 hydrochloride) is a potent and dual ALK/MET inhibitor with IC50s of <0.4 nM and 0.74 nM, respectively. -
Raf kinase inhibitor
B-Raf inhibitor 1 dihydrochloride is a potent Raf kinase inhibitor with Kis of 1 nM, 1 nM, and 0.3 nM for B-RafWT, B-RafV600E, and C-Raf, respectively. -
p38α MAPK inhibitor
MW-150 hydrochloride (MW01-18-150SRM hydrochloride) is a selective, CNS penetrant, and orally active inhibitor of p38α MAPK with a Ki of 101 nM. -
p38α MAPK inhibitor
MW-150 dihydrochloride dihydrate (MW01-18-150SRM dihydrochloride dihydrate) is a selective, CNS penetrant, and orally active inhibitor of p38α MAPK with a Ki of 101 nM. -
p38α MAPK inhibitor
BMS-582949 hydrochloride is an orally active and highly selective p38α MAPK inhibitor, with an IC50 of 13 nM. -
p38 MAPK α/β inhibitor
Ralimetinib (LY2228820) is a potent and selective, ATP-competitive inhibitor of p38 MAPK α/β, with IC50s of 5.3 and 3.2 nM, respectively.
