MAPK
Catalog No.
Product Name
Application
Product Information
Citations
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p38/CK1 Inhibitor
p38α MAPK/CK1δ inhibitor-1 is a selective inhibitor targeting p38α MAPK and CK1δ, exhibiting IC50 values of 0.185 µM and 0.089 µM, respectively. This compound plays a crucial role in modulating cellular responses associated with stress and inflammatory pathways. Its inhibition of both kinases makes it a valuable tool for investigating signaling pathways and therapeutic strategies in various disease models. -
JNK3 Inhibitor
JNK3-IN-10 is a selective inhibitor of JNK3, demonstrating an IC50 value of 0.257 nM and exhibiting over 400-fold selectivity over JNK1. This compound effectively disrupts the JNK3-mediated signaling pathway in response to TGF-β1, leading to the inhibition of c-Jun phosphorylation and a reduction in pro-fibrotic marker expression while restoring E-cadherin levels. Its low cytotoxicity profile, along with anti-fibrotic, cytoprotective, and renoprotective properties, makes JNK3-IN-10 a valuable tool for investigating chronic kidney disease, glomerulosclerosis, and adriamycin-induced nephropathy. -
BChE/p38-α MAPK Inhibitor
BChE/p38-α MAPK-IN-1 is a selective dual inhibitor targeting human butyrylcholinesterase (BChE) with an IC50 of 772 nM and p38 α MAPK with an IC50 of 191 nM. This compound significantly reduces the production of pro-inflammatory cytokines such as IL-1β, IL-6, IL-8, and TNF-α in cellular models. BChE/p38-α MAPK-IN-1 demonstrates the potential to ameliorate cognitive impairments induced by scopolamine and alleviate spatial learning deficits in LPS-treated mice, making it a valuable tool for studying Alzheimer's disease by addressing cholinergic deficits and neuroinflammation. -
HPK1 Inhibitor
HPK1-IN-56 is a potent HPK1 inhibitor with an IC50 of 2.70 nM. It effectively inhibits downstream phosphorylation of SLP76, demonstrating an IC50 of 8.1 nM in Jurkat T cells. This compound induces IL-2 production in human peripheral blood mononuclear cells (PBMCs) and enhances T-cell cytotoxicity, contributing to its anticancer properties. HPK1-IN-56 also improves the antitumor efficacy of anti-PD-1 antibody therapies, making it a valuable tool for cancer immunotherapy research. -
HPK1 Inhibitor
HPK1-IN-64 is a highly selective, orally bioavailable inhibitor of HPK1, featuring an IC50 of 1.9 nM. It demonstrates significant selectivity for HPK1 over GLK, MAP4K5, TBK1, and TNIK, with respective selectivity ratios exceeding 100-fold. This compound effectively inhibits SLP76 protein phosphorylation and reduces IL-2 secretion, making it a valuable tool for investigating signaling pathways in cancer research, particularly colorectal cancer. -
ERK2/STAT3 Activator
Fulipiftide is a short peptide that acts as an activator of the ERK2 and STAT3 signaling pathways. This compound promotes the expansion of nuclear stem cell factor +TSPC, demonstrating significant anti-inflammatory activity. Fulipiftide is particularly useful in research related to acute tendon injury and in studies exploring regenerative medicine and tissue repair mechanisms. -
AP-1/STAT/ERK Inhibitor
Methyllinderone is an inhibitor of the AP-1, STAT, and ERK signaling pathways. This compound exhibits anti-inflammatory properties and has been shown to reduce the invasion and migration rates of TPA-stimulated MCF-7 breast cancer cells. Methyllinderone serves as a valuable tool for research applications focused on breast cancer metastasis and the underlying mechanisms of cancer progression. -
ERK1/2 Inhibitor
Ulixertinib hydrochloride is a potent, orally active inhibitor of the ERK1/2 kinases, functioning primarily through ATP competition and reversible covalent binding. With an IC50 of less than 0.3 nM against ERK2, this compound effectively inhibits phosphorylated ERK2 (pERK) and its downstream target, RSK (pRSK) in A375 melanoma cells. Ulixertinib hydrochloride is valuable for research aimed at understanding the role of ERK signaling in cancer biology and therapeutic strategies targeting this pathway. -
hRKIP-Raf1 Inhibitor
Cefotetan is a selective inhibitor of the human Raf1 kinase inhibitor protein (hRKIP). By binding to hRKIP, Cefotetan reduces its interaction with Raf1 kinase, thereby alleviating the inhibition of the Ras/Raf1/MEK/ERK signaling pathway and facilitating enhanced ERK phosphorylation. This mechanism makes Cefotetan valuable for research on diseases linked to dysregulated signaling within this pathway. Additionally, Cefotetan functions as a broad-spectrum antibacterial agent by binding to bacterial penicillin-binding proteins (PBPs) and disrupting cell wall synthesis, making it useful for investigating bacterial infections, particularly in the contexts of bone, skin, urinary tract, and lower respiratory tract infections. -
ERK Inhibitor
Ravoxertinib hydrochloride is an orally bioavailable inhibitor that selectively targets ERK kinase activity, demonstrating IC50 values of 6.1 nM for ERK1 and 3.1 nM for ERK2. This compound exhibits significant inhibition of ERK signaling pathways, making it a valuable tool for research in cancer biology and targeted therapies. Its selective action on ERK kinases positions it as an important reagent for investigating therapeutic strategies in ERK-driven malignancies. -
BRAF Kinase Inhibitor
Tinlorafenib is a potent inhibitor of BRAF and CRAF kinases, exhibiting IC50 values of 5.8 nM and 4.1 nM, respectively. It specifically targets V600E and V600K mutations in BRAF with IC50s of 4.25 nM and 2.7 nM, making it valuable for studying BRAF-driven tumors. Notably, Tinlorafenib demonstrates effective penetration of the blood-brain barrier, facilitating research into both central nervous system tumors and extracranial malignancies associated with BRAF mutations. -
MEK Inhibitor
Polfurmetinib is a potent MEK inhibitor that selectively targets the MEK signaling pathway. It effectively inhibits the phosphorylation of ERK1/2 at Thr202/Tyr204 in A375 melanoma cells, with an IC50 of 2 nM. This compound is primarily utilized in cancer research to investigate therapeutic strategies that disrupt the MEK/ERK signaling axis. -
p38 MAPK Inhibitor
Chicanine is a lignan derived from Schisandra chinensis that functions as a selective inhibitor of p38 MAPK. It effectively inhibits LPS-induced phosphorylation of p38 MAPK, ERK 1/2, and IκB-α, demonstrating significant anti-inflammatory activity. This compound is valuable for research applications centered around inflammation, signaling pathways, and the modulation of MAPK-related processes. -
ERK Inhibitor
ZINC12409120 is a highly selective ERK inhibitor that targets the mitogen-activated protein kinase pathway. It disrupts the interaction between FGF23 and α-Klotho, leading to inhibition of ERK activity with an IC50 of 5.0 μM. This compound is valuable for research applications focused on cellular signaling pathways and their implications in various disease models. -
ERK1/2 Inhibitor
ERK1/2 Inhibitor 9 is a covalent inhibitor targeting ERK1/2, exhibiting sub-micromolar activity in cellular assays with a GI50 of 0.47 μM in A375 cells. This compound effectively downregulates phospho-ERK1/2 levels, thereby impacting downstream signaling pathways. Additionally, ERK1/2 Inhibitor 9 is functionalized with trans-cyclo-octene (TCO) and Tz-Thalidomide, enabling the formation of ERK-CLIPTAC for targeted degradation of ERK1/2. This makes it a valuable tool for research into cancer signaling mechanisms and targeted protein degradation strategies. -
ERK/JNK Inhibitor
Ambuic acid is a potent inhibitor targeting the ERK/JNK pathway, demonstrating notable anti-inflammatory effects. It displays significant antimicrobial activity against Staphylococcus aureus, with an IC50 value of 43.9 μM for the ATCC 6538 strain. Additionally, Ambuic acid inhibits the biosynthesis of cyclic peptide quorum sensing molecules in gram-positive bacteria, making it a valuable compound for research in antimicrobial and anti-inflammatory applications. -
PROTAC ERK5 Degrader
PPM-3 is a potent and selective PROTAC degrader of ERK5, exhibiting an IC50 of 62.4 nM. While PPM-3 does not directly affect tumor cell proliferation, it modulates tumor development by impacting macrophage differentiation. This compound may serve as a valuable tool for investigating the role of ERK5 degradation in cancer biology and immune modulation. -
ERK2 Inhibitor
ERK2-IN-4 is a selective inhibitor of the ERK2 pathway, demonstrating a Ki of 0.006 μM. This compound effectively disrupts ERK signaling, making it a valuable tool in cancer research. Its specificity and potency allow for detailed studies of ERK2's role in tumorigenesis and related signaling pathways. -
ERK5 Inhibitor
ERK5-IN-5 is an inhibitor of the ERK5 kinase, showcasing significant anti-cancer properties. This compound demonstrates notable anti-proliferative effects, with an IC50 value of 6.23 µg/mL against A549 lung cancer cells. ERK5-IN-5 is suitable for research applications focused on cancer biology and signaling pathways involving ERK5 modulation. -
p38 MAPK Inhibitor
FR 167653 is a selective inhibitor of p38 mitogen-activated protein kinase (MAPK), demonstrating significant suppression of pro-inflammatory cytokines such as TNF-α and IL-1β through targeted inhibition of p38 MAPK activity. This compound is effective in preclinical models for managing inflammation and provides therapeutic benefits in conditions related to trauma and ischemia-reperfusion injury. Its ability to modulate inflammatory responses makes it a valuable tool for research in inflammation and related disorders. -
p38 MAPK Inhibitor
Dilmapimod tosylate is a potent inhibitor of p38 mitogen-activated protein kinase (MAPK), a key regulator of inflammatory responses. This compound exhibits significant biological activity by reducing pro-inflammatory cytokine production, making it a valuable tool in studying inflammatory processes. It has potential applications in researching chronic inflammatory diseases, including chronic obstructive pulmonary disease (COPD). -
p38 MAPK Inhibitor
p38 MAPK-IN-2 is a selective inhibitor of p38 mitogen-activated protein kinase (MAPK). This compound effectively attenuates p38 MAPK signaling, leading to decreased phosphorylation of downstream targets involved in inflammatory responses. It is valuable for researchers studying cellular stress responses, cytokine signaling, and potential therapeutic effects in various inflammatory diseases and cancer. -
p38 MAPK Inhibitor
2-Phenylacetamide is a potent inhibitor of the p38 MAPK signaling pathway. This compound demonstrates significant anti-inflammatory, antioxidant, anti-hypertensive, and anti-fibrotic properties, making it a valuable tool for investigating various biological processes. Additionally, 2-Phenylacetamide is orally active, facilitating its use in in vivo research applications. -
JNK Inhibitor
JNK-9L is an ATP-competitive inhibitor targeting c-Jun N-terminal kinases (JNK1 and JNK3), exhibiting IC50 values of 0.099 and 0.148 μM, respectively. This compound effectively inhibits c-jun phosphorylation and reduces reactive oxygen species (ROS) generation induced by Streptozotocin with an IC50 of 0.8 nM. JNK-9L is particularly relevant for research into neurodegenerative diseases, including Parkinson’s disease, facilitating investigations into the therapeutic modulation of JNK pathways. -
MEK1/2 Inhibitor
U0126 is a selective inhibitor of MEK1 and MEK2, functioning through a non-ATP competitive mechanism. It demonstrates potent biological activity with IC50 values of 72 nM and 58 nM for MEK1 and MEK2, respectively. U0126 is utilized in research to investigate autophagy and mitophagy processes, providing insights into cellular signaling pathways and potential therapeutic targets in cancer and other diseases. -
p38 MAPK Inhibitor
p38 MAPK-IN-1 is a selective inhibitor of p38 MAPK, exhibiting an IC50 of 68 nM. This compound demonstrates sustained plasma levels, low clearance, and favorable bioavailability, making it an effective tool for biological research. p38 MAPK-IN-1 is primarily utilized in studies investigating inflammatory responses, apoptosis, and various disease states involving p38 MAPK signaling pathways. -
p38 MAPK Inhibitor
Doramapimod hydrochloride is a selective inhibitor of p38 MAPK, a key regulator in inflammatory responses. This compound effectively attenuates the production of pro-inflammatory cytokines, including TNF-α and IL-1β, in response to LPS, LTA, and PGN stimulation. Its potent anti-inflammatory properties make Doramapimod hydrochloride valuable for researching various autoimmune diseases and inflammatory pathways. -
P38 MAPK Inhibitor
2-Oleoxyphenethyl phosphocholin is an inhibitor of the p38 MAPK pathway, which plays a critical role in cellular stress responses and inflammatory processes. This compound exhibits significant anticancer activity, potentially through its interaction with the lipid-binding pocket of p38 MAPK. Its broad-spectrum anti-tumor properties make 2-Oleoxyphenethyl phosphocholin a valuable tool for research in cancer biology and therapeutic development. -
p38α MAPK Inhibitor
p38-α MAPK-IN-4 is a selective inhibitor of p38α MAPK, exhibiting an IC50 value of 1.5 µM. This compound demonstrates significant efficacy in the prevention of mechanical allodynia in vivo, making it a valuable tool for research into pain mechanisms and inflammatory responses. Its specificity and potency render it suitable for investigating the role of p38α MAPK in various biological contexts, including neurobiology and chronic pain studies. -
p38α Inhibitor
P38α-IN-11 is a selective inhibitor of p38α, exhibiting a KD value of 586 nM. This compound is primarily utilized in research investigating cervical cancer, enabling studies on the modulation of p38α signaling pathways and their implications in tumorigenesis. Its inhibitory effects make it a valuable tool for elucidating the role of p38α in cancer biology. -
p38 Inhibitor
p38 Kinase Inhibitor 4 is a selective inhibitor of p38 mitogen-activated protein kinase (MAPK), which plays a crucial role in mediating cellular responses to stress and inflammation. This compound demonstrates significant anti-inflammatory activity, making it valuable for research in inflammation-related diseases and cellular signaling pathways. It serves as an essential tool for studying p38 MAPK's role in such processes and evaluating potential therapeutic strategies. -
p38 MAPK Inhibitor
p38 MAPK-IN-9 is a selective inhibitor of p38α mitogen-activated protein kinase (MAPK), demonstrating an IC50 value of 9.6 nM. This compound exhibits potent anti-inflammatory activity, making it a valuable tool for research into inflammatory diseases, including rheumatoid arthritis, septic shock, and chronic obstructive pulmonary disease (COPD). Its oral bioavailability and high selectivity position p38 MAPK-IN-9 as an effective reagent for exploring the role of p38 MAPK in various biological pathways and therapeutic interventions. -
p38 MAPK Inhibitor
AZD 6703 is a selective inhibitor of p38α MAP kinase, targeting the MAPK pathway involved in inflammatory responses. It demonstrates significant anti-inflammatory activity, making it a valuable tool for investigating inflammatory diseases and related therapeutic interventions. Researchers can utilize AZD 6703 to explore p38 MAPK's role in various cellular processes and to develop strategies for modulating inflammation. -
p38 Inhibitor
L-167307 is a potent p38 kinase inhibitor that exhibits anti-inflammatory properties. It has been shown to significantly reduce secondary paw swelling in rat models of adjuvant-induced arthritis. This compound is valuable for research applications involving inflammation and pain pathways, facilitating the study of p38-mediated signaling in various disease models. -
PLK1/p38γ Inhibitor
PLK1/p38γ-IN-1 is a multitarget inhibitor that selectively targets PLK1 and p38γ kinases. This compound has demonstrated the ability to inhibit cell proliferation in human hepatocellular carcinoma and hepatoblastoma cell lines in vitro. PLK1/p38γ-IN-1 is valuable for research focused on cancer biology and the modulation of cell cycle pathways. -
p38 MAPK Inhibitor
Ganoderterpene A is a potent inhibitor of p38 MAPK, demonstrating significant anti-inflammatory and anti-apoptotic activity. It effectively attenuates LPS-induced inflammation and apoptosis by suppressing the MAPK and TLR-4/NF-κB signaling pathways in BV-2 cells. This compound is valuable for research applications focused on neuroinflammation and cellular stress responses. -
P38 MAPK Inhibitor
2-Stearoxyphenethyl phosphocholin is a potent inhibitor of p38 MAPK, a key regulator of inflammatory and stress response pathways. This compound demonstrates significant anticancer activity and may selectively interact with the lipid-binding pocket of p38 MAPK, influencing its function. Due to its broad-spectrum anti-tumor properties and lipid-modulating effects, it is applicable in cancer research and studies focused on metabolic regulation. -
p38α inhibitor
p38-α MAPK-IN-5 is a potent inhibitor of p38α MAPK, exhibiting competitive affinity with an IC50 of 0.1 nM against p38α, and 0.2 nM for p38β, while displaying reduced efficacy toward p38γ and p38δ. This compound demonstrates significant anti-inflammatory properties, making it a valuable tool for researching inflammatory pathways associated with conditions such as asthma and chronic obstructive pulmonary disease (COPD). Its specificity for p38α underscores its potential utility in studies aimed at elucidating the role of this kinase in inflammatory responses and related therapeutic interventions. -
p38 MAP Inhibitor
BIRB-1017 is a selective inhibitor of p38 MAP kinase, a key regulator in the inflammatory response. It demonstrates significant biological activity by modulating cytokine production and cellular signaling pathways associated with inflammation. This compound is suitable for use in research focused on understanding p38 signaling in various inflammatory diseases and therapeutic interventions. -
p38 MAP Kinase Inhibitor
p38 MAPK-IN-10 is a potent inhibitor of p38 MAP kinase, exhibiting an IC50 of 570 nM. This orally active compound shows promise in the study of chronic inflammatory diseases, including rheumatoid arthritis and Crohn’s disease. Its mechanism of action targets the p38 MAPK signaling pathway, making it a valuable tool for researchers investigating therapeutic approaches to modulate inflammation. -
p38α Inhibitor
R-130823 is a highly selective p38α inhibitor that exhibits an IC50 of 22 nM specifically against p38α, with minimal activity towards p38β (IC50 of 820 nM) and no significant interaction with p38γ or p38δ. This compound effectively downregulates cartilage degradation and inflammatory mediators, including the inhibition of MMP-13, MMP-1, and PGE2 release. R-130823 demonstrates therapeutic potential in reducing hind paw swelling, alleviating hyperalgesia, and impeding the progression of arthritis. It is particularly relevant for research studies focusing on osteoarthritis and rheumatoid arthritis. -
p38 Kinase Inhibitor
p38 Kinase Inhibitor 5 (AA6) selectively targets p38 MAP kinase, exhibiting a potent inhibitory effect with an IC50 of 403.57 nM. This compound is known for its significant anti-inflammatory activity, making it a valuable tool for research in inflammatory disease models and studies related to cytokine signaling pathways. Its role in modulating p38 kinase activity can provide insights into the mechanistic understanding of various pathological conditions. -
p38 MAP Kinase/Phosphodiesterase 4 Inhibitor
CBS-3595 is a dual inhibitor of p38 MAP kinase and phosphodiesterase 4, exhibiting potent anti-inflammatory and anti-allodynic effects. This compound significantly decreases the production of the proinflammatory cytokine IL-6 while elevating levels of the anti-inflammatory cytokine IL-10 in rat models. Additionally, CBS-3595 effectively mitigates paw edema in the Complete Freund’s adjuvant-induced arthritis model, making it a valuable tool for investigating potential therapies for autoimmune diseases. -
p38α Inhibitor
p38α inhibitor 7 is a potent inhibitor of the p38α mitogen-activated protein kinase, a key regulator of inflammation and stress responses. This compound demonstrates significant biological activity by effectively modulating the p38α pathway, making it applicable in studies exploring inflammatory diseases and neurological disorders. Its favorable pharmacokinetic properties enhance its potential for oral administration in therapeutic research. -
p38 MAP Inhibitor
AW-814141 is a selective and orally active inhibitor of p38 MAP kinase, demonstrating IC50 values of 100 nM for p38-α and 158 nM for p38-β isoforms. This compound effectively reduces TNF-α production induced by LPS and demonstrates a dose-dependent inhibition of paw edema in rat models. AW-814141 serves as a valuable tool in studying anti-inflammatory mechanisms and has potential applications in researching inflammatory diseases, including rheumatoid arthritis. -
p38αMAPK Inhibitor
MW108 hydrochloride is a selective inhibitor of p38α MAPK, with an affinity (Ki) of 114 nM. This compound demonstrates the ability to mitigate beta-amyloid-induced synaptic impairments and cognitive dysfunction, making it a valuable tool for studying neurodegenerative disorders. Its central nervous system penetration enhances its utility in research focused on Alzheimer's disease and related pathologies. -
p38α-MK2 Inhibitor
p38α-MK2-IN-1 is a potent inhibitor of the p38α-MK2 complex, demonstrating an IC50 of 5 nM. This compound exhibits significant anti-inflammatory properties and promotes joint repair, making it a valuable tool for studies focused on inflammation and regenerative medicine. Researchers can employ p38α-MK2-IN-1 in various applications, including drug discovery and the exploration of signaling pathways related to inflammatory responses. -
p38 Kinase Inhibitor
p38 Kinase-IN-9 is a potent p38 kinase inhibitor characterized by an IC50 of less than 1 μM. This compound is valuable for investigating the role of p38 kinase in various diseases, particularly those related to inflammation. It serves as a useful tool for research applications aimed at understanding the mechanistic pathways of p38-mediated disorders. -
p38α Inhibitor
p38α-IN-9 is a potent p38α inhibitor that effectively suppresses the enzymatic activity of p38α with an IC50 value below 20 nM. This compound inhibits MK2T334 phosphorylation, resulting in the activation of Cdc25b and Cdc25c, while concurrently inactivating Wee1. The modulation of these pathways induces mitotic catastrophe, aneuploidy, and polyploidy, contributing to DNA damage. p38α-IN-9 is particularly relevant in studies of colorectal cancer metastasis. -
p38 MAPK Inhibitor
(aS)-PH-797804 is a selective inhibitor of p38 MAPK, demonstrating IC50 values of 26 nM for p38 α and 102 nM for p38 β. This compound exhibits significant anti-inflammatory activity, making it a valuable tool for research applications focused on inflammatory signaling pathways and related disease models. Its specificity towards p38 MAPK allows for the exploration of its role in cellular processes and therapeutic interventions in conditions associated with p38 MAPK dysregulation.
