MAPK
Catalog No.
Product Name
Application
Product Information
Citations
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ERK2 Inhibitor
ERK-IN-2 free base is a selective inhibitor of ERK2, demonstrating an IC50 value of 1.8 nM. This compound is useful for studying the role of ERK2 in various signaling pathways and cellular processes. Researchers should be mindful of potential off-target toxicity or activity at concentrations exceeding 10 μM, which may impact experimental outcomes. -
ERK Inhibitor
ERK-IN-8 is an aniline pyrimidine derivative that functions as a selective inhibitor of ERK2. It demonstrates potent inhibitory activity with an IC50 of ≤50 nM in vitro. This compound is valuable for applications in cancer research, enabling investigations into ERK signaling pathways and their roles in tumorigenesis. -
SOS1-Ras Inhibitor
UC-857993 is a selective inhibitor of the SOS1-Ras interaction, effectively suppressing its catalytic activity with a Kd of 14.7 μM (His6-SOS1cat). This compound also inhibits ERK and Ras activation, demonstrating significant capabilities in reducing the proliferation of mouse embryonic fibroblasts (MEFs). UC-857993 is valuable for research into cancer biology and signaling pathways involving Ras. -
ERK Inhibitor
Laxiflorin B is a selective inhibitor of ERK1/2, a key component of the MAPK signaling pathway. It exhibits significant antitumor activity, making it a valuable compound for cancer research. Laxiflorin B is particularly useful for investigations into the molecular mechanisms of ERK-related pathways and their roles in oncogenesis. -
ERK Inhibitor
ERK2 IN-5 is a selective inhibitor of ERK2 that demonstrates significant affinity for the target, with a Ki value of 86 nM, as well as for JNK3, with a Ki of 550 nM. This compound is suitable for research applications involving the modulation of ERK signaling pathways, providing a valuable tool for studying cellular processes such as proliferation, differentiation, and apoptosis in various biological contexts. -
ERK2 Inhibitor
ERK2-IN-3 is a selective inhibitor of ERK2, effectively blocking the phosphorylation of both Erk2WT and Erk2DS1 activation loops with IC50 values of 5 μM and 42 nM, respectively. This compound provides valuable insights into the role of ERK2 in various signaling pathways and is applicable in research related to cancer, cell proliferation, and differentiation. ERK2-IN-3 may facilitate the study of ERK signaling and its potential therapeutic interventions. -
ERK1/2 Inhibitor
ERK1/2 Inhibitor 5 is a highly effective inhibitor specifically targeting ERK1/2, members of the mitogen-activated protein kinase (MAPK) family. By interfering with the MAPK signaling pathway, this compound demonstrates significant potential in research applications related to cancer, inflammation, and other proliferative disorders. Its ability to modulate cellular signaling makes it a valuable tool in the study of various pathophysiological conditions. -
Erk1/2 Activator
β-Neo-Endorphin acetate is an endogenous opioid peptide that primarily acts as an Erk1/2 activator. Originating from porcine hypothalamus as a precursor to Leu-enkephalin, it demonstrates significant biological activity by activating Erk1/2, as well as matrix metalloproteinases MMP-2 and MMP-9. This compound is valuable for research focused on neurobiology, pain modulation, and cellular signaling pathways involving opioid receptors. -
ERK2 Inhibitor
ERK2 allosteric-IN-1 is a selective allosteric inhibitor of ERK2, exhibiting an IC50 value of 11 μM. This compound modulates ERK2 activity, providing a valuable tool for investigating the role of ERK1/2 signaling in various biological processes. Its specificity for ERK2 makes it suitable for studies in cancer research, cellular signaling, and related therapeutic applications. -
NF-κB&ERK1/2 Inhibitor
OP-1118 is a potent dual inhibitor of NF-κB and ERK1/2, targeting critical signaling pathways involved in inflammation and cell survival. This compound demonstrates significant anti-inflammatory, cytoprotective, anti-apoptotic, and antibacterial activities by inhibiting the phosphorylation of NF-κB and ERK1/2, leading to a reduction in pro-inflammatory cytokine expression. In preclinical models of Clostridium difficile infection, OP-1118 effectively mitigates toxin-induced intestinal inflammation, cellular damage, and apoptosis, with its protective effects possibly reversible by PMA. This makes OP-1118 a valuable reagent for research into inflammatory conditions and therapeutic interventions. -
ERK Inhibitor
Laxiflorin B-4 is a selective ERK1/2 inhibitor, demonstrating a higher affinity compared to its parent compound, Laxiflorin B. This enhanced binding significantly increases its potential for tumor suppression, making it a valuable tool in cancer research. Laxiflorin B-4 can aid in the study of ERK signaling pathways and their role in oncogenesis. -
KLK-10/ERK Inhibitor
Picrasidine J is a selective inhibitor of KLK-10 protease and the ERK signaling pathway. It demonstrates significant anti-migratory and anti-invasive activities by upregulating E-Cadherin and ZO-1 while downregulating β-catenin and Snail. Additionally, it reduces KLK-10 expression and inhibits ERK phosphorylation. Picrasidine J is primarily utilized in research aimed at preventing metastasis in head and neck squamous cell carcinoma (HNSCC). -
ERK1/2 Inhibitor
ERK1/2 inhibitor 6 is a selective inhibitor targeting extracellular signal-regulated kinases 1 and 2 (ERK1/2), key components of the mitogen-activated protein kinase (MAPK) signaling pathway. This compound exhibits significant activity in modulating signal transduction processes, making it a valuable tool in cancer research, inflammation studies, and the investigation of other proliferative diseases. Its potential applications include elucidating the role of ERK1/2 in cellular processes and exploring therapeutic strategies for related pathologies. -
ERK Inhibitor
Sonvuterkib is a potent inhibitor of extracellular signal-regulated kinases (ERK), demonstrating IC50 values of 1.4 nM for ERK1 and 0.54 nM for ERK2. This orally active compound effectively inhibits cell proliferation, making it a valuable tool in cancer research. Its ability to target ERK signaling pathways highlights its potential for therapeutic applications in various cancer models. -
ERK-MAPK Pathway Inhibitor
ITZ-1 is a selective inhibitor of the extracellular signal-regulated kinase (ERK) in the mitogen-activated protein kinase (MAPK) pathway, exhibiting an IC50 of 0.51 μM against interleukin-1β (IL-1β)-induced matrix metalloproteinase-13 (MMP-13) production. This compound effectively reduces MMP-13 expression and mitigates nitric oxide (NO)-induced chondrocyte apoptosis. ITZ-1 holds potential for advancing research in osteoarticular diseases. -
ERK1/2 Inhibitor
ERK1/2 inhibitor 10 is a highly potent inhibitor of ERK1 and ERK2, exhibiting IC50 values of 0.11 nM and 0.08 nM, respectively. This compound effectively blocks the phosphorylation of downstream substrates, including p90RSK and c-Myc, leading to enhanced cell apoptosis and incomplete autophagy-related cell death. ERK1/2 inhibitor 10 demonstrates significant antitumor activity against triple-negative breast cancer and colorectal cancer models, particularly those with BRAF and RAS mutations, making it a valuable tool for cancer research. -
ERK1/2 Inhibitor
ERK1/2 Inhibitor 12 is a selective inhibitor of the ERK1 and ERK2 signaling pathways. It effectively inhibits ERK-mediated phosphorylation of caspase-9 and p90Rsk-1 kinase, demonstrating significant anti-cancer activity. This compound is suitable for research applications focused on cancer biology and the modulation of ERK signaling in various cellular contexts. -
ERK5 Inhibitor
ERK5-IN-4 is a selective inhibitor of extracellular signal-regulated kinase 5 (ERK5), demonstrating potent activity against both full-length and truncated ERK5 variants. In HEK293 cells, ERK5-IN-4 exhibits inhibitory effects with IC50 values of 77 nM for full-length ERK5 and 300 nM for ERK5 ΔTAD. This compound is valuable for research applications targeting signaling pathways involving ERK5, including studies on cell proliferation, differentiation, and stress response mechanisms. -
ERK5 Inhibitor
ERK5-IN-6 is a kinase inhibitor targeting extracellular signal-regulated kinase 5 (ERK5). This compound demonstrates notable anticancer activity, exhibiting an IC50 value of 4.56 µg/mL against A549 lung cancer cells. ERK5-IN-6 is a valuable tool for research into the role of ERK5 in cancer biology and potential therapeutic applications. -
Erk2 Inhibitor
ETP-45835 dihydrochloride is a selective inhibitor of Erk2, exhibiting an IC50 value of 18.7 μM. This compound demonstrates significant inhibitory effects on cell proliferation, with an EC50 value of 0.9 μM. ETP-45835 is valuable for research applications focused on cell signaling pathways and the modulation of Erk2 activity in various biological contexts. -
ERK2 Inhibitor
Tizaterkib (hexanedioic acid) is a potent and selective inhibitor of ERK2, exhibiting an IC50 of 0.6 nM. This compound effectively disrupts ERK2 signaling pathways, making it valuable for investigating the role of ERK2 in various biological processes. Its application extends to cancer research and drug discovery, providing insights into therapeutic strategies targeting ERK2-associated pathways. -
BRAF PROTACs Negative Control
CG 858-Neg is a negative control for Thalidomide-derived PROTAC degraders targeting BRAF and BRAFV600E, exhibiting Ki values of 9.5 nM and 14.4 nM, respectively. This compound effectively inhibits downstream phosphorylation of ERK and demonstrates suppression of BRAFV600E-driven tumorigenesis in melanoma (A375 cells, IC50 = 492 nM) and colorectal cancer (HT-29 cells, IC50 = 459 nM) models. CG 858-Neg is suitable for research applications focused on the mechanisms of melanoma and colorectal carcinoma. -
ERK1/5 Inhibitor
ADTL-EI1712 is a selective dual-target inhibitor of ERK1 and ERK5, demonstrating inhibition rates of 93.54% and 89.35%, respectively, at a concentration of 1 μM. It effectively induces regulated cell death by activating genetically encoded machinery, making it valuable for research focused on overcoming compensatory mechanisms in specific cancer cells. This compound is suitable for in vitro and in vivo studies exploring therapeutic strategies targeting the ERK signaling pathway. -
Selective p38α Inhibitor
AMG-548 dihydrochloride is a selective p38α inhibitor with a Ki of 0.5 nM, exhibiting moderate selectivity towards p38β (Ki = 36 nM) and over 1000-fold selectivity against p38γ and p38δ isoforms. This compound demonstrates potent inhibition of TNFα production in whole blood stimulated by LPS, with an IC50 of 3 nM. Additionally, AMG-548 dihydrochloride inhibits Wnt signaling by directly targeting Casein kinase 1 isoforms δ and ε, making it valuable for research in inflammation and signaling pathways. -
Selective p38α Inhibitor
AMG-548 hydrochloride is a selective inhibitor targeting p38α with a Ki of 0.5 nM and shows moderate selectivity for p38β (Ki=36 nM), while exhibiting over 1000-fold selectivity against p38γ and p38δ. This compound effectively inhibits TNFα production in whole blood stimulated by LPS, with an IC50 of 3 nM. Additionally, AMG-548 hydrochloride disrupts Wnt signaling through the direct inhibition of Casein kinase 1 isoforms δ and ε, making it a valuable reagent for studies in inflammation and cancer research. -
p38/CK1 Inhibitor
p38α inhibitor 8 selectively inhibits p38α MAPK and CK1δ, with IC50 values of 0.21 µM and 0.202 µM, respectively. This compound is valuable for studies exploring cellular stress responses and inflammatory pathways, making it a potent tool in cancer research and immunology. Its ability to modulate these kinases presents opportunities for investigating therapeutic strategies in various diseases. -
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. -
HPK1 Inhibitor
HPK1-IN-61 is a potent inhibitor of hematopoietic progenitor kinase 1 (HPK1), exhibiting a Ki value of 0.4 nM. Additionally, it demonstrates strong inhibitory activity against Abl with an IC50 of less than 0.51 nM, and LCK with an IC50 of 24 nM. This compound is valuable for research applications focused on immune signaling and kinase regulation. -
BCR-ABL/SRC/p38 Inhibitor
CHMFL-ABL-053 is a potent, selective inhibitor targeting BCR-ABL, SRC, and p38 kinases, exhibiting IC50 values of 70 nM, 90 nM, and 62 nM, respectively. This compound demonstrates significant antiproliferative activity, making it a valuable tool in cancer research, particularly in studies focusing on chronic myeloid leukemia and related malignancies. Its oral bioavailability enhances its utility in in vivo research applications. -
Raf Inhibitor
ML786 is a potent Raf inhibitor with oral bioavailability, demonstrating IC50 values of 2.1 nM for V600EΔB-Raf, 4.2 nM for wild-type B-Raf, and 2.5 nM for C-Raf. Additionally, ML786 exhibits inhibitory effects on Abl-1, DDR2, EPHA2, KDR, and RET, with IC50 values under 0.5 nM, 7.0 nM, 11 nM, 6.2 nM, and 0.8 nM, respectively. This compound is suitable for research applications focused on cancer biology, helping to advance understanding of therapeutic targets within malignancies. -
HPK1 Inhibitor
HPK1-IN-2 dihydrochloride is a potent inhibitor of hematopoietic progenitor kinase-1 (HPK1), exhibiting an IC50 of less than 0.05 μM. This compound also demonstrates inhibitory effects on Lck kinase with an IC50 range between 0.05 μM and 0.5 μM, as well as on Flt3, with an IC50 of less than 0.05 μM. Its biological activity and targeted inhibition make HPK1-IN-2 dihydrochloride a valuable tool for research focused on antitumor mechanisms and kinase pathway analyses. -
PDGFRβ/B-Raf Inhibitor
KG5 is an orally active dual inhibitor targeting PDGFRβ and B-Raf through allosteric mechanisms. It also exhibits inhibitory effects on Flt3, KIT, and c-Raf. KG5 demonstrates significant anticancer and antiangiogenic activities, making it a valuable reagent for research in cancer therapy and angiogenesis studies.
