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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.

  • 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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  • 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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  • 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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  • Beta-Tocopherol
    TN1441148-03-8
    Beta-Tocopherol has effects on human erythroleukemia cell (HEL) adhesion induced by phorbol 12-myristate 13-acetate (PMA).
    • $54
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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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  • 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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  • 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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  • 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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  • 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.
    • $69
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  • Takinib
    T42641111556-37-6
    Takinib (EDHS-206) is a specific and effective TAK1 inhibitor(IC50= 9.5 nM).
    • $66
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  • Norisoboldine
    T5S189523599-69-1
    1. Norisoboldine ((+)-Laurelliptine) might be a potential therapeutic agent for rheumatoid arthritis, and it functions through protecting joint destruction as well as regulating the abnormal immune responses. 2. Norisoboldine inhibits the macrophage activation and the resultant production of pro-inflammatory cytokines via down-regulating the activation of MAPKs signaling pathways rather than NF-κB.
    • $60
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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.
    • $33
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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.
    • $30
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  • MBM-55
    T119602083622-09-5
    MBM-55 is an effective inhibitor of NIMA related kinase 2 (NEK2) with an IC50 of 1 nM. MBM-55 effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis.
    • $187
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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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  • GNE-3511
    T37071496581-76-0
    GNE-3511 is a potent and selective dual leucine zipper kinase inhibitors.
    • $45
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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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  • 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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  • NG25
    T56431315355-93-1
    NG25 is a potent dual inhibitor of TAK1 and MAP4K2, with IC50s of 149 nM and 21.7 nM, respectively.
    • $79
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  • NCB-0846
    T40111792999-26-8
    NCB-0846 is an orally active TNIK inhibitor (IC50: 21 nM).
    • $31
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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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  • Pan-RAS-IN-1
    T164321835283-94-7
    Pan-RAS-IN-1 is an inhibitor of pan-Ras. It disrupts the interaction of Ras proteins and their effectors.
    • $73
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  • Semapimod tetrahydrochloride
    T35593164301-51-3
    Semapimod tetrahydrochloride (CPSI-2364 tetrahydrochloride) is a synthetic ornithine mitogen-activated protein kinase blocker and pro-inflammatory cytokine production inhibitor that interferes with macrophage and microglia function. Sematimod tetrahydrochloride inhibits TLR4 signaling, TNF-α, IL-1β, and IL-6, and is used in the study of Crohn's disease and other inflammatory conditions.
    • $99
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  • PF-3644022
    T165011276121-88-0
    PF-3644022 is an effective, selective, and ATP-competitive MAPKAPK2 (MK2) inhibitor (IC50: 5.2 nM and a Ki of 3 nM). PF-3644022 potently inhibits TNFα production and has an anti-inflammatory effect. PF-3644022 also inhibits MK3 and p38 regulated activated
    • $119
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  • Zeylenone
    TN2328193410-84-3
    Zeylenone, a cyclohexene oxide from Uvaria grandiflora, has antitumour and antiproliferative activity, inhibiting cervical cancer cell proliferation and inducing apoptosis through the PI3K AKT mTOR and MAPK ERK signalling pathways.
    • $598
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  • NMS-P715
    T122371202055-32-0
    NMS-P715 is a selective and ATP-competitive MPS1 inhibitor(IC50 of 182 nM).
    • $72
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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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  • GNE-495
    TQ00791449277-10-4
    GNE-495 is a potent and specific inhibitor of MAP4K4 with an IC50 of 3.7 nM.
    • $66
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  • TAK1-IN-3
    T40577494772-87-1
    TAK1-IN-3 is a novel ATP-competitive TAK1 inhibitor for the study of cancer.
    • $46
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  • SM1-71
    T366802088179-99-9
    SM1-71 is a potent multi-targeted acrylamide-modified TAK1 inhibitor that inhibits MKNK2, MAP2K1 2 3 4 6 7, GAK, AAK1, BMP2K, MAP3K7, MAPKAPK5, GSK3A B, MAPK1 3, SRC, YES1, FGFR1, ZAK (MLTK), MAP3K1, LIMK1 and RSK2.SM1-71 can be used as a kinase probe with anticancer activity and inhibits the proliferation of various cancer cell lines.
    • $44
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  • ASK1-IN-2
    T93772541792-70-3
    ASK1-IN-2 is a potent, orally active inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with an IC50 of 32.8 nM. It has potential therapeutic applications for ulcerative colitis[1].
    • $68
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  • MK2-IN-3
    T9034724711-21-1
    MK2-IN-3 (MK2 Inhibitor III) is a potent, cell-permeable inhibitor of mitogen-activated protein kinase-activated protein kinase 2 (MAPKAP-K2 or MK-2) and can be used for the treatment of rheumatoid arthritis
    • $55
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  • Nomilin
    T36721063-77-0
    Nomilin is naturally occurring triterpenoids, have immunomodulatory activity.
    • $39
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  • A-443654
    T14072552325-16-3
    A-443654, a pan-Akt inhibitor, exhibits equal potency against Akt1, Akt2, and Akt3 within cells (Ki=160 pM).
    • $84
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  • MAP4K4-IN-3
    T119421811510-58-3
    MAP4K4-IN-3 (Compound 17), a serine threonine protein kinase, may be a viable target for antidiabetic agents.
    • $39
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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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  • 3',4',7-Trihydroxyisoflavone
    TN1236485-63-2
    3',4',7-Trihydroxyisoflavone is a soy isoflavone soy glycoside derivative and Cot (Tpl2 MAP3K8) and MKK4 inhibitor with anticancer, antiangiogenic and free radical scavenging properties.3',4',7-Trihydroxyisoflavone enhances memory effects through modulation of cholinergic function and BDNF signaling pathway in mice.3',4',7-Trihydroxyisoflavone can improve skin barrier function impaired by endogenous or exogenous glucocorticoids and can be used in the study of atopic dermatitis. 3',4',7-Trihydroxyisoflavone enhances memory effects by modulating cholinergic function and BDNF signaling pathway in mice. It can improve the skin barrier function impaired by endogenous or exogenous glucocorticoids, and can be used in the study of atopic dermatitis.
    • $35
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  • GS-444217
    T51901262041-49-5
    GS-444217 is a selective ATP-competitive inhibitor of apoptosis signal-regulating kinase 1 (ASK1, IC50: 2.87 nM).
    • $40
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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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  • NF-κB/MAPK-IN-1
    T631192413940-56-2
    NF-κB/MAPK-IN-1 is a potent dual inhibitor of the NF-κB and MAPK pathways with potential anti-inflammatory activity, inhibition of NO production, and inhibition of LPS-induced activation of iNOS, COX-2, ERΚ and P38. NF-κB/MAPK-IN-1 is used for the prevention and treatment of rheumatoid arthritis (RA).
    • $39
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  • HS-243
    T60012848249-10-5
    HS-243 is an inhibitor of IRAK-4 and IRAK-1 with IC50s of 20 and 24 nM. HS-243 shows anti-inflammatory and anticancer activity.
    • $30
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  • Bisabolangelone
    TN144530557-81-4
    Bisabolangelone has anti-tumor, anti-inflammatory, anti-microbial, and antioxidant activities, it inhibits dendritic cell functions by blocking MAPK and NF-κB signaling.
    • $44
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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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  • 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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  • TAO Kinase inhibitor 1
    T16987850467-66-2
    TAO Kinase inhibitor 1 delays mitosis and induces mitotic cell death. TAO Kinase inhibitor 1 is a selective and ATP-competitive thousand-and-one amino acid kinases inhibitor (IC50s: 11 to 15 nM for TAOK1 and 2, respectively).
    • $64
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  • ZINC05007751
    T9880591239-68-8
    ZINC05007751 is an effective inhibitor of NIMA-related kinase NEK6 (IC50 = 3.4 μM). ZINC05007751 is very selective against NEK1 and NEK6 with no significant activity observed against NEK2, NEK7, and NEK9.
    • $31
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  • HPK1-IN-4
    T403502739844-28-9
    HPK1-IN-4 is an HPK1 (MAPK41) inhibitor with an IC 50 of 0.061 nM. HPK1-IN-4 is often used as a preclinical immunotherapy tool compound.
    • $132
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  • APS-2-79 hydrochloride
    T67602002381-31-7
    APS-2-79 hydrochloride (APS-2-79 HCl) is a MAPK antagonist that modulating KSR-dependent MAPK signalling by antagonizing RAF heterodimerization as well as the conformational changes required for phosphorylation and activation of KSR-bound MEK.
    • $37
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  • Sodium lauryl sulfoacetate
    T36031847-58-1
    Sodium lauryl sulfoacetate (Sodium houttuyfonate) is anti-pseudomonas agents, inhibits virulence-related motility of Pseudomonas.
    • $30
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  • sodium lauroyl-α-hydroxyethyl sulfonate
    T7283
    Sodium houttuyfonate is anti-pseudomonas agents, inhibits virulence-related motility of Pseudomonas.
    • $32
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