ERK

The activity of Pluripotin (SC-1) is mediated by the combined inhibition of RasGAP and ERK1 with Kd values of 98 and 212 nM, respectively.

XMD8-92 is a potent and selective BMK1/ERK5 inhibitor .

Varenicline Tartrate(CP 526555;Champix) is a nicotinic receptor partial agonist; it stimulates nicotine receptors more weakly than nicotine itself does.

VRT752271 is a pyrrole inhibitors of ERK protein kinase.

trans-Zeatin is a member of the plant hormone family known as ??cytokinins??, which regulate cell division, development, and nutrient processing.

ONO 2506 inhibits S100B synthesis in activated cultured astrocytes.

TCS ERK 11e (VX-11e) is a potent and selective extracellular signal-related kinase 2 (ERK2) inhibitor (Ki values are <2, 395, 540 and 852 nM for ERK2, GSK-3, Aurora Kinase A and Cdk2 respectively). Potently blocks proliferation of HT29 cells (IC50 = 48 nM).

SCH772984 is a novel, specific inhibitor of ERK1/2 with IC50 of 4 nM and 1 nM, respectively.

2',5'-Dihydroxyacetophenone (DHAP, 2-Acetylhydroquinone, Quinacetophenone) is a mixture of dihydroxyacetophenone isomers is used in food flavouring. 2',5'-Dihydroxyacetophenone significantly inhibits NO production via the suppression of iNOS expression. 2',5'-Dihydroxyacetophenone significantly decreases levels of the pro-inflammatory cytokines TNF-α and IL-6 by blocking the ERK1/2 and NF-κB signaling pathways.

GDC-0994 is a potent and selective Erk1/2 inhibitor. GDC-0994 inhibits both ERK phosphorylation and activation of ERK-mediated signal transduction pathways.

BAY885 is a novel ERK5 inhibitor.

MCB has been shown to inhibit both casein kinase 2 (CK2) and extracellular-signal-regulated kinase 8 (ERK8/MAPK15) (IC50 = 0.50 uM for both CK2 and ERK8).

XMD17-109 is a novel, specific inhibitor of ERK-5 with an EC50 value of 4.2 uM in HEK293 cells.

FR 180204 is a novel and selective inhibitor of extracellular signal-regulated kinase (ERK), which may be a potential new therapy for rheumatoid arthritis.

DEL-22379 is a potent and selective ERK Dimerization inhibitor that inhibits ERK Dimerization without affecting ERK phosphorylation, forestalls tumorigenesis driven by RAS-ERK pathway oncogenes.

APS-2-79 is an antagonist of MEK phosphorylation by RAF through direct binding of the KSR active site.

ERK5-IN-1 exhibits potent inhibition of ERK5 with cellular EC50 values of 0.19 uM and enzymatic IC50 values of 0.087 uM and of LRRK2[G2019S] with enzymatic IC50 values of 0.026uM.

Tomatidine inhibits the phosphorylation of ERK, Akt, and the nuclear content of NF-kB. possess anti-inflammatory properties.

CC-90003 is an irreversible inhibitor of ERK1/2 with IC50s in the 10-20 nM range and shows good kinase selectivity in a 258-kinase biochemical assay.

MK-8353 (SCH900353) is an orally bioavailable, selective, and potent ERK inhibitor that inhibits activated ERK1 and ERK2 in vitro, with IC50 values of 23.0 nM and 8.8 nM, respectively (IMAP kinase assay), and nonactivated ERK2, with an IC50 of 0.5 nM (MEK1-ERK2-coupled assay).

AZD0364 is a pre-clinical ERK1/2 inhibitor with an IC50 of 0.6 nM for ERK2.

LY3214996 is a selective and novel ERK1/2 inhibitor with IC50 of 5 nM for both enzymes in biochemical assays. It potently inhibits cellular phospho-RSK1 in BRAF and RAS mutant cancer cell lines.

AG-126 is a ERK2 inhibitor that selectively inhibits the phosphorylation of ERK1 (p44) and ERK2 (p42) at 25-50 μM.

4-Methylbenzylidene camphor(4-MBC; Enzacamene)is an organic camphor derivative that is used in the cosmetic industry for its ability to protect the skin against UV, specifically UV B radiation.

Xanthocillin is a marine agent extracted from Penicillium commune, induces autophagy through inhibition of the MEK/ERK pathway.

ERK5-IN-2 is an orally active, sub-micromolar, selective ERK5 inhibitor with IC50s of 0.82 μM, 3 μM for ERK5 and ERK5 MEF2D, respectively.

Rineterkib (ERK-IN-1) (compound B) is a RAF and ERK1/2 inhibitor in the treatment of a proliferative disease characterized by activating mutations in the MAPK pathway.

CCT020312 is a selective EIF2AK3/PERK activator. CCT020312 elicits EIF2A phosphorylation in cells.

ERK2 IN-1 is a selective ERK2 inhibitor with an IC50 of 7 nM.

ERK1/2 inhibitor 1 is a potent, orally bioavailable ERK1/2 inhibitor, showing 60% inhibition at 1 nM and an IC50 of 3.0 nM against ERK1 and ERK2, respectively.

KO-947 is a potent and selective inhibitor of ERK1/2 kinases with potential clinical utility in MAPK pathway dysregulated tumors.

AX-15836 is a potent and selective ERK5 inhibitor with an IC50 of 8 nM.

TBHQ (tert-Butylhydroquinone) is a widely used Nrf2 activator, protects against Doxorubicin (DOX)-induced cardiotoxicity through activation of Nrf2.

Omtriptolide (PG490-88) is a water soluble derivative prodrug of triptolide purified from the Chinese herb

Urolithin B is one of the gut microbial metabolites of ellagitannins, and has anti-inflammatory and antioxidant effects. Urolithin B is also a regulator of skeletal muscle mass.

Methylthiouracil is an antithyroid agent. Methylthiouracil suppresses the production TNF-α and IL-6, and the activation of NF-κB and ERK1/2.

Pyridoxal 5′-phosphate monohydrate is the active coenzyme form of vitamin B6 and is essential for the function of numerous enzymes. It serves as a key cofactor for aromatic L-amino acid decarboxylase, which catalyzes the final step in the biosynthesis of the neurotransmitters dopamine and serotonin. Pyridoxal 5′-phosphate is the primary intracellular phosphorylated form of vitamin B6 and is interconvertible with other forms, including pyridoxine 5′-phosphate (PNP) and pyridoxamine 5′-phosphate (PMP).

Isofraxidin is a coumarin compound derived from *Acanthopanax senticosus* that exhibits anti-invasive and anti-inflammatory properties. It inhibits MMP-7 expression and suppresses cell invasion in human hepatoma cells by reducing ERK1/2 phosphorylation. Isofraxidin also downregulates the expression of iNOS and COX-2 and inhibits the formation of the TLR4/myeloid differentiation protein-2 (MD-2) complex.

Cafestol is an orally active diterpenoid and an inhibitor of ERK2. It exhibits multiple biological activities, including elevation of blood lipids, anti-inflammatory, anti-angiogenic, and anti-diabetic effects. Additionally, cafestol induces apoptosis and autophagy in tumor cells, making it a potential candidate for cancer research.

Lipoteichoic acid is an orally active compound with anti-inflammatory and antitumor properties. It is a key immune molecule found in Gram-positive bacteria that activates the complement system by upregulating C3 and inhibiting CD55. Lipoteichoic acid modulates macrophage autophagy via the PI3K/Akt/mTOR pathway, induces lung injury in mouse models, and inhibits melanin production.

FR900359 is a cyclic depsipeptide and a selective inhibitor of Gαq/11/14 proteins in mammals. By targeting Gαq signaling, it effectively inhibits downstream pathways such as the ERK cascade. FR900359 has demonstrated the ability to suppress melanoma cell proliferation, lower blood pressure, and protect against airway hyperreactivity in murine models of allergen sensitization, such as the ovalbumin-induced asthma model.

C16-PAF (PAF (C16)) is a phospholipid mediator and a potent platelet-activating factor that functions as a ligand for the PAF G-protein-coupled receptor (PAFR). It exhibits anti-apoptotic effects by inhibiting caspase-dependent cell death through PAFR activation. C16-PAF is a strong activator of the MAPK and MEK/ERK signaling pathways and is known to induce increased vascular permeability.

Edaxeterkib is a potent inhibitor of extracellular signal-regulated kinase (ERK), designed for cancer research. By targeting the ERK signaling pathway, Edaxeterkib interferes with tumor cell proliferation and survival, making it a valuable tool for studying ERK-driven malignancies.

ABD56 is a bioactive compound that inhibits osteoclast formation and induces osteoclast apoptosis. Its mechanism of action involves suppression of the NFκB and ERK signaling pathways, making it a promising candidate for research in bone metabolism and osteolytic diseases.

Lobeglitazone sulfate is a novel thiazolidinedione and an orally active agonist of peroxisome proliferator-activated receptors (PPARs), with EC50 values of 137.4 nM for PPARγ and 546.3 nM for PPARα. It also acts as an inhibitor of the ERK/JNK/Smad/NF-κB signaling pathways. Lobeglitazone sulfate exhibits anti-inflammatory, anti-diabetic, anti-fibrotic, and anti-atherosclerotic activities, supporting its potential in the treatment of metabolic and inflammatory diseases.

Hydrangenol is an orally active antiphotoaging compound isolated from *Hydrangea serrata* leaves. It prevents wrinkle formation by downregulating matrix metalloproteinases (MMPs) and inflammatory cytokines, while upregulating moisturizing factors and antioxidant gene expression, making it a promising agent for skin health and anti-aging research.

26-Deoxyactein, a bioactive constituent isolated from *Cimicifuga racemosa*, protects against TCDD-induced osteoblast damage. It exerts its effects by inhibiting the upregulation of aryl hydrocarbon receptor (AhR), CYP1A1, and ERK signaling, making it a potential agent for bone health and toxicology research.

6-Demethoxytangeretin is a flavonoid compound isolated from *Citrus reticulata* with demonstrated anti-inflammatory and anti-allergic properties. It inhibits IL-6 production and the expression of related genes in human mast cells by modulating the ALK and MAPK signaling pathways. Additionally, 6-Demethoxytangeretin enhances CRE-mediated transcription in hippocampal neurons, indicating potential neuroregulatory effects.

Larixol is an fMLP inhibitor that also suppresses key signaling pathways involved in immune regulation, including Src kinase, ERK1/2, p38, and AKT phosphorylation. It disrupts the interaction between the βγ subunit of the fMLP receptor Gi protein and downstream effectors, thereby inhibiting fMLP-induced respiratory burst. Larixol effectively inhibits fMLP (0.1 μM)-induced superoxide anion production (IC50: 1.98 μM), cathepsin G release (IC50: 2.76 μM), and neutrophil chemotaxis. It mitigates neutrophil hyperactivation and helps reduce inflammation and tissue damage. Additionally, Larixol derivatives have shown inhibitory activity against TRPC6 functional mutants associated with focal segmental glomerulosclerosis (FSGS).

Gardenin A is an orally active synthetic polymethoxyflavone (PMF) analogue with neurotrophic properties, promoting neurite outgrowth and neuronal differentiation. It enhances neuritogenesis through activation of the MAPK/ERK, PKC, and PKA pathways, independent of TrkA and CREB signaling. Additionally, Gardenin A exhibits sedative, anxiolytic, antidepressant, and anticonvulsant effects, making it a promising compound for neurological and neuropsychiatric research.