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MAPK

A mitogen-activated protein kinase (MAPK or MAP kinase) is a type of protein kinase that is specific to the amino acids serine and threonine (i.e., a serine/threonine-specific protein kinase). MAPKs are involved in directing cellular responses to a diverse array of stimuli, such as mitogens, osmotic stress, heat shock and proinflammatory cytokines. They regulate cell functions including proliferation, gene expression, differentiation, mitosis, cell survival, and apoptosis.

  • Beta-Tocopherol
    TN1441148-03-8
    Beta-Tocopherol shows effect on human erythroleukemia cell (HEL) adhesion induced by phorbol 12-myristate 13-acetate (PMA).
    • $54
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  • sodium lauroyl-α-hydroxyethyl sulfonate
    T7283
    Sodium houttuyfonate is anti-pseudomonas agents, inhibits virulence-related motility of Pseudomonas.
    • $53
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  • MBP MAPK Substrate acetate
    T38796L
    MBP MAPK Substrate acetate can be used as an exogenous substrate for MAPK.
    • $266
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  • Cot inhibitor-1 hydrochloride
    T10865L In house
    Cot inhibitor-1 hydrochloride is an inhibitor of tumor progression loci-2 kinase (IC50 = 28 nM) and inhibits the production of TNF-α in human whole blood (IC50 = 5.7 nM).
    • $127
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  • SKLB-163
    T261931255099-06-9In house
    SKLB-163 acts by downregulating RhoGDI, activating JNK-1 signaling pathway and caspase-3, and reducing phosphorylated Akt and p44/42 MAPK.
    • $137
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  • MBM-55S
    T119612083624-07-9In house
    MBM-55S is an effective inhibitor of Nek2 with an IC50 of 1 nM. MBM-55S indecus cell cycle arrest and apoptosis thereby inhibiting the proliferation of cancer cells. MBM-55S shows antitumor activities.
    • $195
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  • (R)-STU104
    T606572767124-77-4
    (R)-STU104 is a novel TAK1-MKK3 protein-protein interaction (PPI) inhibitor that inhibits TNF-α and suppresses the TAK1/MKK3/p38/MnK1/MK2/elF4E signalling pathway by binding to MKK3 and disrupting TAK1 phosphorylation of MKK3. (R)-STU104 is a candidate compound for the treatment of ulcerative colitis.
    • $195
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  • Gardenin A
    TN411421187-73-5
    Gardenin A shows neurotrophic effects via activating MAPK/ERK, PKC, and PKA. Gardenin A exhibits antidepressant, anticonvulsant and anxiolytic effects.
    • $197
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  • methyl 5-(3,4-dimethoxyphenyl)isoxazole-3-carboxylate
    T8911517870-17-6
    methyl 5-(3,4-dimethoxyphenyl)isoxazole-3-carboxylate is a biochemical.
    • $50
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  • PAF (C16)
    T2154774389-68-7In house
    PAF (C16) is a potent MAPK and MEK ERK activator that induces increased vascular permeability. PAF (C16) (PAF (C16)) is a platelet-activating factor, a phospholipid-derived mediator and a ligand for PAF G protein-coupled receptor (PAFR). PAF (C16) has shown anti-apoptotic and anti-inflammatory activity in vitro, inhibiting Caspase-dependent apoptosis by interacting with its receptor (PAF-R) to perform cell signaling.
    • $67
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  • Cot inhibitor-2
    T10866915363-56-3In house
    Cot inhibitor-2 is a cot (Tpl2/MAP3K8) inhibitor (IC50: 1.6 nM) with potency, selectivity and oral activity. cot inhibitor-2 inhibits LPS-stimulated TNF-α production in human whole blood with an IC50 of 0.3 μM.
    • $93
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  • Cot inhibitor-1
    T10865915365-57-0In house
    Cot inhibitor-1 is a selective inhibitor of Cot protein kinase (also known as Tpl2 or MAP3K8) (IC50 at 28 nM). Cot inhibitor-1 inhibited TNF-alpha production in human whole blood with IC50 of 5.7 nM. Cot is involved in a variety of cellular signaling pathways, particularly those involved in inflammation and immune responses. Cot inactivate-1 inhibits Cot activity and may have potential therapeutic effects on rheumatoid arthritis, inflammatory bowel disease and some types of cancer.
    • $70
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  • TC ASK 10
    T130991005775-56-3In house
    TC ASK 10 is a potent, selective and orally active inhibitor of apoptosis signal-regulating kinase 1 (ASK1)(IC50 of 14 nM).
    • $52
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  • GNE-1858
    T114382680616-96-8In house
    GNE-1858 is an ATP-competitive hematopoietic progenitor kinase-1 (HPK1) inhibitor (IC50s of 1.9 nM, 1.9 nM, and 4.5 nM for wild-type and the active mimetic mutants HPK1-TSEE and HPK1-SA).
    • $175
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  • DMX-5804
    T54832306178-56-1
    DMX-5804 is a potent, selective MAP4K4 inhibitor, with an IC50 of 3 nM.DMX-5804 enhances cardiomyocyte survival, and reduces ischemia-reperfusion injury in mice.
    • $108
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    TargetMol | Citations Cited
  • Takinib
    T42641111556-37-6
    Takinib (EDHS-206) is a specific and effective TAK1 inhibitor(IC50= 9.5 nM).
    • $66
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  • Vemurafenib
    T2382918504-65-1
    Vemurafenib (RG7204) is a B-RAF inhibitor that inhibits RAFV600E and c-RAF-1 (IC50=31/48 nM) selectively and potently. Vemurafenib exhibits antitumor activity and is used for the treatment of BRAF V600E mutation-positive melanoma.
    • $50
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  • PF-06260933
    T42211811510-56-1
    PF-06260933 is a highly selective small-molecule MAP4K4 inhibitor with IC50s of 3.7 and 160 nM for kinase and cell, respectively.
    • $42
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  • Eudesmin
    T3836526-06-7
    Eudesmin shows antiinflammatory, neuritogenic, anticonvulsant and sedative effects, the mechanism of eudesmin may be related to up-regulation of GABAA and GAD65 expressions, and anti-apoptosis of neuron the in brain.50 microM (+)-eudesmin can induce neurite outgrowth and enhance nerve growth factor (NGF)-mediated neurite outgrowth from PC12 cells by stimulating up-stream MAPK, PKC and PKA pathways.
    • $142
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  • Rehmannioside A
    T378881720-05-0
    Rehmannioside A, a cyclic enol ether terpene glycoside extracted from the traditional Chinese medicine Dihuang, possesses neuroprotective activity and acts by inhibiting NF-κB and MAPK signaling pathways.
    • $68
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  • NQDI-1
    T3101175026-96-7
    NQDI-1 (NQDI 1) is a selective inhibitor of apoptosis signal-regulating kinase 1 (ASK1, MAP3K5) (IC50/Ki: 3 μM/500 nM).
    • $40
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  • Selonsertib
    T33501448428-04-3
    Selonsertib (GS-4997) is an orally bioavailable inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with potential anti-inflammatory, antineoplastic and anti-fibrotic activities.
    • $45
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  • BI-3406
    T129792230836-55-0
    BI-3406 is an orally active, highly potent and selective between KRAS and Son of Sevenless 1 (SOS1) interaction inhibitor(IC50 : 6 nM),with anticancer activity.
    • $67
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  • NG25
    T56431315355-93-1
    NG25 is a potent dual TAK1 and MAP4K2 inhibitor, with IC50s of 149 nM and 21.7 nM, respectively.
    • $79
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  • Flavokawain C
    TN164556798-34-6
    Flavokawain C is a melanogenesis inhibitor, it inhibited melanogenesis with IC50 values of 6.9 μM. Flavokawain C has anti-tumor activity, it inhibited cell cycle and promoted apoptosis, associated with endoplasmic reticulum stress and regulation of MAPKs and Akt signaling pathways in HCT 116 human colon carcinoma cells.
    • $2,080
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  • Zunsemetinib
    T391261640282-42-3
    Zunsemetinib (ATI-450) is an orally active and selective inhibitor of the p38α mitogen-activated protein kinase-activated protein kinase 2 (MK2) pathway.Zunsemetinib is used to study spondyloarthritis and rheumatoid arthritis.
    • $283
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  • HS220
    T600111570374-32-1
    HS220 is an inhibitor of TAK1 which plays a key role in the signaling pathways of inflammation and cell survival.
    • $75
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  • Antimicrobial agent-21
    T67942724746-07-0
    Antimicrobial agent-21 is a potent mitogen activated protein kinase inhibitor with antibacterial, anti-inflammatory and antitumor activity for the treatment of cataracts, ulcerative colitis, meningitis and Kawasaki's disease and Parkinson's disease.
    • $123
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  • Communic acid
    TN36912761-77-5
    Communic acid has antibacterial activity, including against mycobacterial. trans-Communic acid has potential to be utilized as anti-wrinkling agents and cosmetic ingredients, as they suppress UVB-induced MMP-1 expression.
    • $460
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  • Manassantin A
    TN448988497-87-4
    Manassantin A is a high potent HIF-1 inhibitor, it protects the gastric mucosa from ethanol-induced acute gastric injury, and suggest that these protective effects might be associated with COX/PGE2 stimulation, inhibition of iNOS production and NF-κB act
    • $1,280
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  • CMPD1
    T1498841179-33-3
    CMPD1 is a non-ATP-competitive p38 MAPK-mediated MK2 phosphorylation inhibitor(apparent Ki (Kiapp): 330 nM).
    • $44
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  • Picrasidine I
    TN4785100234-59-1
    Picrasidine I has antiosteoclastogenic effect by inhibiting inflammation induced activation of MAPKs, NF-κB and ROS generation followed by suppressing the gene expression of c-Fos and NFATc1 in osteoclast precursors.
    • $1,920
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  • MK2-IN-3 hydrate
    T120581186648-22-5
    MK2-IN-3 hydrate (MK-2 Inhibitor III) is an orally active, selective, and ATP-competitive inhibitor of MAPKAP-K2 (MK-2) (IC50 of 0.85 nM)
    • $48
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  • Ganoderic acid X
    TN410786377-53-9
    Ganoderic acid X is a potential Mdm2 inhibitor(K(i) = 16nM). It is a potential anticancer drug, inhibits topoisomerases and induces apoptosis of cancer cells.
    • $290
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  • Gallocatechin gallate
    TN40945127-64-0
    Gallocatechin gallate has strong antioxidative, and anti-obesity activities, it inhibits 3T3-L1 differentiation and lipopolysaccharide induced inflammation through MAPK and NF-κB signaling; it also may have anti-diabetic effects by increasing sensitivity
    • $80
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  • Dehydrogeijerin
    TN380516850-91-2
    Dehydrogeijerin significantly inhibits the inflammatory activity of activated macrophages, suggesting that it could be a potential candidate for the treatment of inflammatory disease.
    • $590
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  • Capillarisin
    TN358756365-38-9
    Capillarisin is a novel blocker of STAT3 activation and thus may have a potential in negative regulation of growth, metastasis, and chemoresistance of tumor cells, it inhibits cancer cell growth of osteosarcoma cells by inducing apoptosis accompanied with
    • $2,169
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  • Taspine
    TN5100602-07-3
    Taspine shows antitumor activity by modulating the EGFR signaling pathway of Erk1/2 and Akt in vitro and in vivo, it can inhibit growth and induce apoptosis of HUVEC in a dose-dependent manner, it has shown meaningful angiogenesis activity. Taspine exhibi
    • $540
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  • Isojacareubin
    TN430050597-93-8
    Isojacareubin displays potent activity against H. pylori HP40 clinical isolate with MIC 23.9 uM, which is approximately two times greater than that of the standard drug amoxicillin. Isojacareubin is a potent inhibitor of protein kinase C (PKC), suppresses
    • $2,068
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  • CC-99677
    T393211887069-10-4
    CC-99677 (Gamcemetinib) is a selectively targeted covalent MAPKAPK2 (MK2) inhibitor for autoimmune diseases that translates biochemical potency into cellular potency as demonstrated by potent inhibition of heat shock protein 27 (HSP1) phosphorylation in LPS-activated monocyte THP-27 cells via a nucleophilic aromatic substitution (SNAr) mechanism.CC-99677 in Rat experiments demonstrated potency in both biochemical (IC 50 =156.3 nM) and cellular assays (EC 50 =89 nM).
    • $123
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  • Aristolactam AIIIa
    TL001797399-91-2
    Aristolactam AIIIa is a new type of Plk1 inhibitors, targeting the Polo Box domain (PBD), it has anti-tumor activity. Aristolactam IIIa shows inhibition of platelet aggregation induced by collagen or arachidonic acid.
    • $2,710
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  • HS-276
    T622092767422-72-8
    HS-276 is a highly selective, orally active inhibitor of TAK1 (Ki: 2.5 nM). HS-276 significantly inhibits TAK1 (IC50: 8.25 nM), CLK2 (IC50: 29 nM), GCK (IC50: 22 nM), ULK2 (IC50: 63 nM), MAP4K5 (IC50. HS-276 can be used to study rheumatoid arthritis (RA).
    • $91
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  • Scandoside
    TN495618842-99-4
    Scandoside, a cyclic enolide that can be isolated from Haemophilus difficile, exhibits anti-inflammatory activity, inhibits the expression levels of inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2), TNF-α, and IL-6 messenger RNA (mRNA), and inhibits the nuclear transcription factor, kappa-B alpaha (IκB-α), p38, extracellular signal-regulated kinase (ERK) and c-Jun N-terminal kinase (JNK) inhibitor phosphorylation.
    • $540
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  • Momordin Ic
    T341096990-18-0
    Momordin Ic (Momordin 1c) might represent a potential anticancer activity, by inducing apoptosis through oxidative stress-regulated mitochondrial dysfunction involving the MAPK and PI3K-mediated iNOS and HO-1 pathways. Also, Momordin Ic accelerates gastrointestinal transit partially by stimulating synthesis of 5-HT to act through 5-HT(2), which, in turn, increases synthesis of prostaglandins.
    • $80
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  • 5Z-7-Oxozeaenol
    T14055253863-19-3
    5Z-7-Oxozeaenol (FR148083) is a potent, irreversible and selective inhibitor of transforming growth factor (TGF)-β-activated kinase 1 with IC50 of 8.1 nM for TAK1 and low activity against MEK1 with IC50 of 411 nM, it is also an inhibitor of VEGF-R2 with IC50 of 52 nM.
    • $215
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  • Gossypetin
    TN1711489-35-0
    Gossypetin, a hexahydroxylated flavonoid extractable from Rhodiola rosea Linn. is a potent MKK3 and MKK6 inhibitor that strongly attenuates the MKK3 6-p38 signaling pathway.Gossypetin exhibits antimutagenic, antiatherosclerotic, antioxidant, as well as cytoprotective and antimicrobial effects.It inhibits bone resorption by downregulating lysosomal caspase K activity and inducing autophagy-associated proteins in actin ring osteoclasts. Gossypetin has anti-mutagenic, anti-atherosclerotic, anti-oxidant, cytoprotective and antibacterial effects, and it inhibits bone resorption by down-regulating lysosomal caspase K activity and by inducing autophagy-associated protein in actin ring osteoblasts.
    • $222
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  • GNE-495
    TQ00791449277-10-4
    GNE-495 is a potent and specific MAP4K4 inhibitor (IC50: 3.7 nM).
    • $66
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  • 2,3-Dihydro-3-methoxywithaferin A
    TN269421902-96-5
    2,3-Dihydro-3-methoxywithaferin A is a natural withanolide , is cytotoxic to human cancer cells, and is a candidate anticancer natural compound. It protects normal cells against stress.
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  • MK2-IN-1 hydrochloride
    T44421314118-94-9
    MK2-IN-1 hydrochloride (MK 25) is a highly selective, non-ATP competitive inhibitor of p38/mitogen-activated protein kinase-activated protein kinase 2 (MAPKAPK2 or MK2, IC50: 0.11 μM) [1].
    • $32
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  • Isonardosinone
    TN431527062-01-7
    Isonardosinone shows potential role in the treatment of neuroinflammation conditions, it inhibits NF-κB- and MAPK-mediated inflammatory pathways.
    • $510
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