MAPK

Beta-Tocopherol shows effect on human erythroleukemia cell (HEL) adhesion induced by phorbol 12-myristate 13-acetate (PMA).

Sodium houttuyfonate is anti-pseudomonas agents, inhibits virulence-related motility of Pseudomonas.

MBP MAPK Substrate acetate can be used as an exogenous substrate for MAPK.

SKLB-163 acts by downregulating RhoGDI, activating JNK-1 signaling pathway and caspase-3, and reducing phosphorylated Akt and p44/42 MAPK.

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).

(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.

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.

Gardenin A shows neurotrophic effects via activating MAPK/ERK, PKC, and PKA. Gardenin A exhibits antidepressant, anticonvulsant and anxiolytic effects.

methyl 5-(3,4-dimethoxyphenyl)isoxazole-3-carboxylate is a biochemical.

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.

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.

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.

TC ASK 10 is a potent, selective and orally active inhibitor of apoptosis signal-regulating kinase 1 (ASK1)(IC50 of 14 nM).

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).

Takinib (EDHS-206) is a specific and effective TAK1 inhibitor(IC50= 9.5 nM).

PF-06260933 is a highly selective small-molecule MAP4K4 inhibitor with IC50s of 3.7 and 160 nM for kinase and cell, respectively.

NQDI-1 (NQDI 1) is a selective inhibitor of apoptosis signal-regulating kinase 1 (ASK1, MAP3K5) (IC50/Ki: 3 μM/500 nM).

Selonsertib (GS-4997) is an orally bioavailable inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with potential anti-inflammatory, antineoplastic and anti-fibrotic activities.

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.

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.

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.

Scandoside exerts anti-inflammatory effect via suppressing NF-κB and MAPK signaling pathways in LPS-induced RAW 264.7 macrophages.It also inhibits LDL-oxidation.

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.

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.

Ganoderic acid C1 has anti-inflammatory activity, has potential for treating TNF-α± mediated inflammation in asthma and other inflammatory diseases. Ganoderic acid C1 has anti-tumor-promoting activity. It is moderately active inhibitors against HIV-1 prot

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.

HS220 is an inhibitor of TAK1 which plays a key role in the signaling pathways of inflammation and cell survival.

NMS-P715 is a selective and ATP-competitive MPS1 inhibitor(IC50 of 182 nM).

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)

CMPD1 is a non-ATP-competitive p38 MAPK-mediated MK2 phosphorylation inhibitor(apparent Ki (Kiapp): 330 nM).

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.

Dehydrogeijerin significantly inhibits the inflammatory activity of activated macrophages, suggesting that it could be a potential candidate for the treatment of inflammatory disease.

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

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.

ASK1-IN-2 is a potent and orally active inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with an IC50 of 32.8 nM. ASK1-IN-2 can potentially be used as a therapeutic strategy for ulcerative colitis[1].

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

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.

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

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

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.

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.

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.

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.

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.

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.

GNE-495 is a potent and specific MAP4K4 inhibitor (IC50: 3.7 nM).

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).

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).

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.

Isonardosinone shows potential role in the treatment of neuroinflammation conditions, it inhibits NF-κB- and MAPK-mediated inflammatory pathways.