MAPK
Catalog No.
Product Name
Application
Product Information
Citations
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MEK Inhibitor
L-783277 is a potent MEK inhibitor with an IC50 of 4 nM, demonstrating significant inhibition against various kinases, including VEGFR2/3, FLT1/3/4, KDR, and PDGFRα. Although it exhibits low selectivity within its kinase targets, L-783277 effectively reduces cell viability and proliferation in H295R cells, with IC50 values of 22 μM and 21 μM, respectively. This compound is applicable in cancer research, particularly in the study of adrenocortical carcinoma. -
ERK/Insulin Receptor Inhibitor
ERK Inhibitor II (Negative Control) is a selective inhibitor of extracellular signal-regulated kinase (ERK) primarily affecting the insulin receptor pathway. This compound serves as a tool for investigating the role of ERK in various biological processes, particularly in the research of diabetes and insulin signaling mechanisms. Its application extends to studying the modulation of ERK activity and understanding associated cellular responses. -
MEK1/2 Inhibitor
SMK-17 is a selective, non-ATP-competitive inhibitor of MEK1 and MEK2, exhibiting IC50 values of 62 nM and 56 nM, respectively. By binding to the allosteric pocket of MEK1/2, SMK-17 effectively modulates the MAPK signaling pathway. This compound demonstrates significant biological activity by inducing apoptosis in tumor cell lines with β-catenin mutations, making it a valuable tool for cancer research and therapeutic investigations targeting these mutations. -
B-Raf Inhibitor
INU-152 is a potent and selective inhibitor of B-Raf, a key kinase in the MAPK signaling pathway. This compound effectively reduces tumor cell proliferation, enhances autophagy, and induces apoptosis through the inhibition of B-Raf activity. INU-152 demonstrates significant cytotoxicity against cancer cells transformed with v-Ha-ras (Ras-NIH 3T3), making it a valuable tool for cancer research applications. -
JNK Inhibitor
Cyy-272 is a potent orally active inhibitor of c-Jun N-terminal kinase (JNK), exhibiting IC50 values of 1.25 μM for JNK1, 1.07 μM for JNK2, and 1.24 μM for JNK3. This compound demonstrates significant anti-inflammatory properties by inhibiting JNK phosphorylation, effectively mitigating acute lung injury induced by lipopolysaccharide. Additionally, Cyy-272 reduces inflammation in cardiomyocytes and cardiac tissues affected by high lipid concentrations, contributing to decreased cardiac hypertrophy, fibrosis, and apoptosis. It is valuable for research into the mechanisms of obese cardiomyopathy and related cardiovascular disorders. -
TAK1 Inhibitor
Triptriolide is a TAK1 inhibitor that plays a pivotal role in regulating apoptosis in mouse podocytes. It enhances cell survival and protects podocyte function by modulating the Bcl-2 family proteins and inhibiting Caspase-3 activity. Additionally, Triptriolide activates the TAK1-NF-κB signaling pathway, leading to the upregulation of podocin. This reagent is relevant for studies focusing on kidney health and podocyte resilience under stress conditions. -
ERK1/2 Inhibitor
Methyl helicterate is a triterpenoid compound that functions as an inhibitor of the ERK1/2 signaling pathway. It demonstrates significant biological activity by inhibiting hepatic stellate cell activation and promoting apoptosis in these cells. This manipulation of the ERK1/2 pathway positions methyl helicterate as a valuable reagent for research focused on liver fibrosis and related conditions. -
p38/CK1 Inhibitor
Casein kinase 1δ-IN-29 is a potent inhibitor of p38α and casein kinase 1, demonstrating IC50 values of 0.041 µM for p38α, 0.005 µM for CK1δ, and 0.447 µM for CK1ε. This compound effectively interrupts the cell cycle at the subG1 phase and induces apoptosis in AC1-M88 cells. It serves as a valuable tool in research applications focused on cell cycle regulation and apoptosis pathways. -
B-Raf Inhibitor
B-Raf IN 9 is a potent B-Raf inhibitor with an IC50 of 24.79 nM, targeting the B-Raf signaling pathway. This compound induces apoptosis and causes cell cycle arrest at the G2/M phase. B-Raf IN 9 demonstrates significant antitumor activity against the human prostate cancer PC-3 cell line, with an IC50 of 7.83 µM, making it a valuable tool for cancer research and therapeutic investigations. -
Estrogen Receptor Agonist, Voltage-Gated Sodium Channel Blocker, PI3K-AKT/JNK Signaling Modulator,
Propylparaben sodium acts as a weak estrogen receptor agonist and serves as a voltage-gated sodium channel blocker, while also modulating the PI3K-AKT and JNK signaling pathways. It is known to induce oxidative stress, affecting the estrous cycle and hormone levels, as well as ovarian reserve function. Propylparaben sodium can inhibit the growth of antral follicles and influence the accumulation of steroid hormones in follicle culture media. This compound is suitable for research related to ovarian aging and myocardial ischemia-reperfusion injury. -
ERK1/2 Inhibitor
ERK1/2 inhibitor 13 is a potent dual inhibitor of ERK1 and ERK2, exhibiting IC50 values of 91.71 nM and 97.87 nM, respectively. This compound demonstrates significant activity in inhibiting the proliferation of tumor cell lines, including MCF-7, 4T1, MDA-MB-468, and HCC1970, with IC50 values ranging from 0.67 to 2.76 μM. Additionally, ERK1/2 inhibitor 13 effectually inhibits cancer cell migration and induces apoptosis and autophagy in MCF-7 cells, while also displaying antitumor and anti-metastatic properties in a 4T1 xenograft mouse model, making it a valuable reagent for cancer research applications. -
ERK1/2 Inhibitor
SF-3-030 is a selective, non-ATP competitive inhibitor of ERK1/2, targeting the MAPK signaling pathway. It has demonstrated the ability to induce apoptosis specifically in melanoma cells with mutated BRAF and activated ERK1/2 signaling. Additionally, SF-3-030 has shown potential in alleviating several characteristics of asthma in murine models, making it valuable for research focused on both melanoma and asthma pathophysiology. -
JNK2/3 Inhibitor
YL5084 is a covalent inhibitor targeting JNK2 and JNK3, demonstrating selectivity for these isoforms with IC50 values of 70 nM and 84 nM, respectively, while showing significantly reduced activity against JNK1 at 2173 nM. This compound exhibits JNK2-independent antiproliferative effects and effectively induces apoptosis without reliance on JNK2 pathways. YL5084 serves as a valuable tool for research into cellular signaling and cancer biology, particularly in studies focusing on the role of JNK isoforms in tumor growth and survival. -
TOPK Inhibitor
SKLB-C05 is a highly selective, orally active inhibitor of the T-Lymphokine-Activated Killer Cell-originated Protein Kinase (TOPK), exhibiting an IC50 of 0.5 nM. This compound has demonstrated the ability to induce apoptosis, downregulate c-Myc, and activate p53 while disrupting FAK/Src-mediated migratory signaling. Additionally, SKLB-C05 interferes with cell mitosis and displays significant anticancer activity specifically against TOPK-positive colorectal cancer, making it a valuable tool for cancer research. -
JNK3 Inhibitor
JNK3 inhibitor-5 is a selective inhibitor targeting JNK3, exhibiting a potent IC50 of 0.379 nM. This compound demonstrates significant neuroprotective activity by safeguarding neuronal cells from amyloid beta-induced apoptosis. Additionally, JNK3 inhibitor-5 is characterized by high cell permeability and is predicted to effectively cross the blood-brain barrier, making it a valuable tool for studying neurological disorders and related therapeutic applications. -
EGFR/BRAFV600E Inhibitor
EGFR/BRAFV600E-IN-1 is a potent dual inhibitor targeting EGFR and the BRAFV600E mutation, with IC50 values of 0.08 µM and 0.15 µM, respectively. This compound effectively induces apoptosis and induces cell cycle arrest in the pre-G1 and G2/M phases. Additionally, it demonstrates significant antiproliferative activity against A-549, MCF-7, Panc-1, and HT-29 cell lines, with IC50 values of 1.2 µM, 0.79 µM, 1.3 µM, and 1.23 µM, respectively, making it valuable for cancer research focused on these targets. -
TLR4/JNK/NF-κB Inhibitor
TLR4-IN-2 is an inhibitor targeting TLR4, JNK, and NF-κB pathways. It demonstrates anti-inflammatory properties by reducing nitric oxide production in LPS-stimulated RAW264.7 cells, with an IC50 of 23.2 µM. By inhibiting TLR4 expression and diminishing JNK phosphorylation, TLR4-IN-2 effectively suppresses NF-κB activation and the transcription of inflammation-related genes, leading to lower levels of iNOS, COX-2, and various inflammatory mediators. This compound shows potential for investigating therapeutic strategies in inflammatory diseases such as rheumatoid arthritis and other inflammatory disorders. -
TNIK/MAP4K4 Inhibitor
Rentosertib is an orally active inhibitor of TNIK and MAP4K4, exhibiting IC50 values of 12-120 nM for both targets. This compound plays a crucial role in the modulation of signaling pathways involved in cell proliferation and survival. Relying on its potent inhibition, rentosertib is utilized in research applications exploring cancer biology and potential therapeutic interventions for related disorders. -
HPK1 Inhibitor
GNE-6893 is a selective inhibitor of HPK1, demonstrating a Ki of less than 0.02 nM. This compound enhances T cell receptor signaling and promotes IL-2 production in stimulated primary human T cells, making it valuable for the investigation of T cell activation mechanisms. GNE-6893 is particularly relevant for research applications focused on chronic refractory cancers. -
HPK1 Inhibitor
AZ3246 is a selective inhibitor of HPK1, exhibiting an IC50 of less than 3 nM. This compound promotes IL-2 secretion in T cells, with an EC50 of 90 nM, highlighting its immunomodulatory properties. AZ3246 serves as a valuable tool for research in cancer biology, particularly in the study of breast cancer therapeutics. -
HPK1 Inhibitor
HPK1-IN-68 is a potent inhibitor of hematopoietic progenitor kinase 1 (HPK1), with an IC50 value of 2.8 nM. This compound effectively blocks HPK1 signaling pathways, inhibits the phosphorylation of SLP76, and stimulates the production of the IL-2 cytokine. Additionally, HPK1-IN-68 counteracts the immunosuppressive effects of prostaglandin E2 (PGE2) and promotes the infiltration of CD3+/CD8+ T cells into tumor microenvironments, demonstrating T cell-dependent antitumor activity in a mouse colon cancer model. It is particularly relevant for research into colon cancer therapeutics. -
Pan-RAF Inhibitor
SJ-C1044 is a pan-RAF inhibitor that demonstrates both immunomodulatory and anti-tumor properties. This compound effectively targets wild-type BRAF, wild-type CRAF, and BRAF (V600E) with IC50 values of 331, 257, and 187 nM, respectively, leading to inhibition of Kras activation and MEK-ERK phosphorylation, which reduces tumor cell proliferation. Additionally, SJ-C1044 exhibits inhibitory effects on VEGFR2, TIE2, and CSF1R, with IC50 values of 100, 23, and 235 nM, respectively, contributing to the improvement of the tumor immune microenvironment via the inhibition of angiogenesis and modulation of macrophage function. SJ-C1044 is suitable for research applications in colorectal cancer studies. -
BRAF/VEGFR2 Inhibitor
Takeda-6D is a potent and orally active inhibitor targeting BRAF and VEGFR2, displaying IC50 values of 7.0 nM and 2.2 nM, respectively. This compound effectively suppresses angiogenesis by inhibiting the VEGFR2 signaling pathway in 293/KDR and VEGF-stimulated HUVEC cells. Additionally, Takeda-6D demonstrates significant inhibition of ERK1/2 phosphorylation, indicating its potential for antitumor activity in various cancer research applications. -
SRC/Raf/VEGFR2 Inhibitor
SKLB646 is a multi-target kinase inhibitor with a focus on SRC, Raf, and VEGFR2. It exhibits potent inhibitory activity against SRC and VEGFR2, with IC50 values of 0.002 μmol/L and 0.012 μmol/L, respectively, as well as significant effects on B-Raf and C-Raf. SKLB646 disrupts SRC signaling and inhibits the MAPK pathway by targeting Raf kinases, leading to decreased proliferation, migration, and invasion in human umbilical vein endothelial cells (HUVEC), thereby impeding tumor-induced angiogenesis. It also demonstrates significant anti-proliferative and anti-survival effects on triple-negative breast cancer (TNBC) cell lines, making it a valuable tool for cancer research. -
p38 MAPK Inhibitor
JNJ-49095397 is a selective inhibitor of p38 MAPK, targeting both the α and γ isoforms. This compound also exhibits inhibition of the SRC kinase family, particularly haematopoietic kinase (HCK). JNJ-49095397 demonstrates significant anti-inflammatory activities and is utilized in research focused on chronic obstructive pulmonary disease (COPD) and asthma. -
p38MAPK Inhibitor
SB 220025 is a selective inhibitor of p38 MAPK, operating through an ATP-competitive mechanism with an IC50 of 60 nM. This compound is effective in reducing the expression of the IL-8 gene in response to globular adiponectin, thereby decreasing inflammatory cytokine production and inhibiting angiogenesis. Additionally, SB 220025 demonstrates efficacy in preventing arthritis progression within chronic inflammatory disease models, making it a valuable tool for research on inflammation and related pathologies. -
RET/BRAF/S6K/Src Inhibitor
AD57 is an orally active multikinase inhibitor that targets RET, BRAF, S6K, and Src, effectively reducing mTOR activity. This compound demonstrates significant biological activity by interfering with critical signaling pathways involved in cancer proliferation and survival. AD57 is suitable for research applications focused on cancer biology and therapeutic development against malignancies driven by these kinases. -
P38-α/Syk Inhibitor
TOP1362 is a potent inhibitor targeting P38-α and Syk kinases, with Kd values of 26 nM and 18 nM, respectively. The compound demonstrates an IC50 of 14 nM in Src kinase activity assays, showcasing its efficacy in inhibiting P38-α, Src, and Syk. TOP1362 is applicable in research focused on dry eye syndrome and related pathways. -
RET/BRAF/S6K/Src Inhibitor
AD57 hydrochloride is a multikinase inhibitor that targets RET, BRAF, S6K, and Src pathways. This orally active compound demonstrates significant biological activity in modulating aberrant signaling pathways associated with various cancers. Research applications include studying the effects of combined inhibition on tumor growth and resistance mechanisms in cancer cell lines and animal models. -
p38MAPK Inhibitor
SB 220025 (tri(hydrochloride)) is a reversible, orally active, ATP-competitive inhibitor of human p38 MAPK, with an IC50 of 60 nM. This compound also exhibits inhibition of p56Lck and PKC with IC50 values of 3.5 μM and 2.89 μM, respectively. SB 220025 trihydrochloride effectively reduces IL-8 gene expression in response to globular adiponectin and diminishes inflammatory cytokine production, making it a valuable tool for studying inflammation and angiogenesis. Additionally, it has shown efficacy in preventing the progression of arthritis in chronic inflammatory disease models. -
JNK/c-Met Inhibitor
JNK-IN-16 is a potent inhibitor of both JNK and c-Met, exhibiting IC50 values of 72 nM and 120 nM, respectively. This compound demonstrates significant anti-cancer activity, making it valuable for research in cancer biology and therapeutic development. Its dual inhibition profile allows for exploration in signaling pathways associated with tumor progression and metastasis. -
BTK/MNK Dual Inhibitor
QL-X-138 is a selective dual inhibitor of Bruton's tyrosine kinase (BTK) and MAPK-interacting kinase (MNK), demonstrating potent covalent binding to BTK and non-covalent binding to MNK. It exhibits IC50 values of 9.4 nM for BTK, and 107.4 nM and 26 nM for MNK1 and MNK2, respectively. Additionally, QL-X-138 displays antiviral activity against dengue virus serotype 2, with an IC50 of 3.5 μM. This compound is valuable for research involving B-cell malignancies and related therapeutic investigations. -
MAPKAPK2 Inhibitor
MK2-IN-1 is a selective inhibitor of MAPKAPK2 (MK2), exhibiting an IC50 of 0.11 µM. This compound significantly interferes with the phosphorylation of serine residues in Tfcp2l1, with an EC50 of 0.35 µM for phosphorylated HSP27. MK2-IN-1 serves as a valuable tool for studying the role of MK2 in cellular signaling pathways and its implications in various biological processes. -
p38/Hsp Activator
Iroxanadine sulfate is a dual activator of p38 kinase and heat shock protein (HSP), functioning as a vasculoprotector. This compound exhibits significant biological activity relevant to vascular health and has potential applications in the study of atherosclerosis and other vascular diseases. Researchers may utilize Iroxanadine sulfate to explore therapeutic strategies aimed at modulating p38 and HSP signaling pathways in various models of vascular pathology. -
TAK1/MAP4K2 Inhibitor
NG25 trihydrochloride is a potent dual inhibitor of TAK1 and MAP4K2, exhibiting IC50 values of 149 nM and 21.7 nM, respectively. This compound enhances the sensitivity of breast cancer cells to Doxorubicin, promoting apoptotic processes. NG25 trihydrochloride serves as a valuable tool for investigating therapeutic strategies in various cancer research applications. -
MAP4K4 Inhibitor
MAP4K4-IN-7 is a selective inhibitor of MAP4K4 that demonstrates moderate inhibitory activity against TNIK, MAP4K4, and MINK1, with pIC50 values of 6.8, 6.8, and 6.7, respectively. This compound can be utilized in research focused on cancer and neurological disorders, including conditions such as schizophrenia. Its ability to modulate MAP4K4 activity makes it a valuable tool for exploring therapeutic strategies in related pathologies. -
HPK1 Inhibitor
ZYF0033 is a potent inhibitor of hematopoietic progenitor kinase 1 (HPK1), achieving an IC50 of less than 10 nM by inhibiting the phosphorylation of MBP protein. This compound enhances anti-cancer immune responses, leading to a reduction in serine 376 phosphorylation of SLP76. In preclinical studies with the 4T-1 syngeneic mouse model, ZYF0033 demonstrated significant tumor growth inhibition and increased intratumoral infiltration of dendritic cells, natural killer cells, and CD107a+CD8+ T cells, while decreasing infiltration of various PD-1+ and TIM-3+ CD8+ T cell subsets. -
HPK1 Inhibitor
HPK1-IN-3 is a potent and selective ATP-competitive inhibitor of hematopoietic progenitor kinase 1 (HPK1; MAP4K1), exhibiting an IC50 of 0.25 nM. The compound demonstrates significant IL-2 potency, with an EC50 of 108 nM in human peripheral blood mononuclear cells (PBMCs). This makes HPK1-IN-3 a valuable tool for investigating the role of HPK1 in immune modulation and cellular signaling pathways. Its targeted inhibition offers potential applications in the study of hematopoietic cell functions and autoimmune disorders. -
HPK1 Inhibitor
DS21150768 is a selective inhibitor of HPK1, a key regulator of T-cell activation. This compound enhances T-cell function and may exhibit potential anticancer effects by modulating immune responses. DS21150768 is suitable for research applications focused on cancer immunotherapy and T-cell biology. -
MAP4K4 Inhibitor
MAP4K4-IN-3 is a potent and selective inhibitor of MAP4K4, exhibiting an IC50 of 14.9 nM in kinase assays and 470 nM in cellular assays. This compound demonstrates significant antidiabetic activity, making it a valuable tool for research in diabetes and metabolic disorders. Its specific action on the MAP4K4 pathway allows for detailed investigation of its biological effects and potential therapeutic applications. -
MAP4K Inhibitor
Famlasertib is a potent inhibitor of MAP4K, specifically targeting HGK (MAP4K4), MLK3, and MLK1 with IC50 values of 0.3 nM, 23.7 nM, and 44.7 nM, respectively. This compound demonstrates neuroprotective and anti-inflammatory effects, making it a valuable tool in research focused on amyotrophic lateral sclerosis (ALS). Famlasertib's ability to penetrate the blood-brain barrier enhances its potential for exploring therapeutic interventions in neurodegenerative diseases. -
HPK1 Inhibitor
HPK1-IN-32 is a potent and selective inhibitor of HPK1, exhibiting an IC50 of 65 nM. This compound is valuable for investigating HPK1-related disorders and diseases, making it an essential tool for research applications targeting cellular signaling pathways associated with immune responses and inflammation. -
HPK1 Inhibitor
HPK1-IN-7 is a potent inhibitor of hematopoietic progenitor kinase 1 (HPK1, MAP4K1) with an IC50 of 2.6 nM, demonstrating excellent selectivity among kinases. It exhibits some selectivity against IRAK4 and GLK, with IC50 values of 59 nM and 140 nM, respectively. This compound has shown significant efficacy in the MC38 syngeneic tumor model, particularly when used in combination with anti-PD1 therapy, highlighting its potential in immuno-oncology research. -
HPK1/GLKb Inhibitor
HPK1/GLK-IN-1 is an inhibitor targeting HPK1 and GLK, demonstrating potent inhibition of GLK with an IC50 value of 33 nM. This compound is primarily utilized in research focused on the modulation of HPK1/GLK signaling pathways, making it a valuable tool for studying animal pathogen infections and related biological mechanisms. Its specificity and potency provide researchers with an effective means to explore therapeutic interventions targeting these kinases. -
HPK1 Inhibitor
GNE-1858 is a highly potent inhibitor of hematopoietic progenitor kinase-1 (HPK1), acting through ATP-competitive mechanisms with IC50 values of 1.9 nM for wild-type HPK1 and 4.5 nM for the active mimetic mutant HPK1-SA. Its remarkable selectivity and efficacy make it an invaluable tool for studying HPK1-related pathways in cellular signaling. GNE-1858 has potential applications in cancer research and immunology, particularly in the modulation of T cell responses and hematopoiesis. -
MAP4K Inhibitor
GNE 220 hydrochloride is a potent and selective inhibitor of MAP4K4, exhibiting an IC50 of 7 nM. This compound demonstrates significant inhibitory activity against MAP4K4, making it a valuable tool for research focused on signaling pathways involved in cellular processes such as differentiation, proliferation, and apoptosis. GNE 220 is particularly relevant for studies investigating the role of MAP4K4 in various diseases, including cancer and inflammatory disorders. -
HPK1 Inhibitor
HPK1-IN-4 is a highly potent inhibitor of HPK1 (MAPK41), exhibiting an IC50 value of 0.061 nM. This compound serves as a valuable tool in preclinical immunological research, facilitating the study of HPK1's role in immune signaling pathways. Its specificity and efficacy make it an essential reagent for investigating therapeutic targets in immune-related disorders. -
HPK1 Inhibitor
HPK1-IN-34 is an inhibitor of Hematopoietic progenitor kinase 1 (HPK1), exhibiting an IC50 of less than 100 nM. This compound serves as a valuable tool in the study of HPK1's role in cellular signaling and immune response. Additionally, HPK1-IN-34 features a terminal alkyne group, enabling its application in click chemistry through copper-catalyzed azide-alkyne cycloaddition (CuAAc), facilitating the conjugation with azide-functionalized molecules for various biochemical studies. -
MAP4K4 Inhibitor
Pyrrolo[2,1-f][1,2,4]triazin-4-amine is an inhibitor of MAP4K4, demonstrating a Kd of 88 μM as assessed by surface plasmon resonance (SPR), with a ligand efficiency of 0.56. This compound is valuable for studies investigating the roles of MAP4K4 in cellular signaling and disease pathways. Its inhibitory properties make it suitable for biochemical assays and potential therapeutic research involving MAP4K4 modulation. -
HPK1 Inhibitor
HPK1-IN-19 is a selective inhibitor of hematopoietic progenitor kinase 1 (HPK1), a critical regulator in various cellular processes, including immune responses and cell proliferation. This compound exhibits significant potential in modulating HPK1 activity, making it valuable for research in immunology and cancer biology. Its ability to impact signaling pathways may provide insights into therapeutic strategies for diseases involving dysregulated HPK1 function.
