ERK Activator

Cearoin increases autophagy and apoptosis through the production of ROS and the activation of ERK.

B7-33 is a single-chain relaxin mimetic and a selective relaxin receptor 1 (RXFP1) agonist. B7-33 phosphorylates ERK1/2 without inducing activation of the cAMP signaling pathway. B7-33 exhibits anti-fibrotic and cardioprotective activities. B7-33 can be used in the research of vascular diseases such as cardiomyopathy, myocardial infarction and fibrosis.

[Tyr8] Bradykinin is a B₂ kinin receptor agonist. [Tyr8] Bradykinin also stimulates ERK1/2 phosphorylation. [Tyr8] Bradykinin can be used as an internal standard.

9 (10)-Nitrooleate (9(10)-Nitrated oleic acid) is an endogenous lipid signaling mediator with vasoprotective effects. 9 (10)-Nitrooleate enhances enzymatic activity and improves nitric oxide bioavailability by inducing phosphorylation of Akt and ERK1/2, regulating the multi-site phosphorylation status of eNOS and optimizing its interaction with Hsp90. 9 (10)-Nitrooleate also activates PPARα, PPARδ and PPARγ receptors, thereby regulating adipogenesis, glucose uptake and inflammation-related gene expression, and exhibits immunosuppressive effects by inhibiting neutrophil migration and cytokine secretion. 9 (10)-Nitrooleate is widely used in studies of sepsis and related inflammatory diseases.

Acifran (AY 25712) is an orally active, full GPR109A and GPR109B agonist and hypolipidemic agent. Acifran reduces Forskolin (HY-15371)-induced cAMP elevation, triggers ERK1/ERK2 phosphorylation, and inhibits lipolysis in adipose tissue through G_i-coupled GPCR activation. Acifran is used for research on atherosclerosis, hyperlipidemia, and type 2 diabetes.

Salbutamol-d₃ (Albuterol-d₃) is the deuterium labeled Salbutamol (HY-B1037). Salbutamol (Albuterol) is an orally active short-acting β2-adrenergic receptor agonist. Salbutamol promotes tumorigenesis in gastric cancer cells through the β2-AR/ERK/EMT pathway. Salbutamol can relax bronchial smooth muscle and is used to study bronchospasm induced by asthma and chronic obstructive pulmonary disease.

Brophenexin free base (compound 8) is a potent NMDAR/TRPM4 interaction interface inhibitor. Brophenexin free base shows neuroprotective activity. Brophenexin free base prevents NMDA-induced cell death and mitochondrial dysfunction in hippocampal neurons, with an IC₅₀ of 2.1 μM. Brophenexin free base protects mice from MCAO-induced brain damage and NMDA-induced retinal ganglion cell loss.

Gardenin A is an orally active and synthetic PMF analogue with the neurotrophic effect for neurite outgrowth and neuronal differentiation. Gardenin A promotes neuritogenesis via activating MAPK/ERK, PKC, and PKA, but not TrkA, CREB signaling pathways. Gardenin A also has sedative, anxiolytic, antidepressant, and anticonvulsant effects.

Famotidine (Standard) (MK-208 (Standard)) is the analytical standard of Famotidine (HY-B0377). This product is intended for research and analytical applications. Famotidine (MK-208) is an orally active and highly selective histamine H2 receptor antagonist. It inhibits gastric acid secretion by blocking the Gs signaling pathway, and regulates intracellular cAMP and ERK pathways. Famotidine inhibits TLR3-mediated inflammatory pathways, and reduces the expression of various inflammatory mediators and interferon-related genes. Famotidine scavenges DPPH and nitric oxide free radicals, alleviates oxidative stress damage in gastric tissue, inhibits proMMP-9, improves vascular endothelial permeability, and restores the normal physiological functions of neutrophils and eosinophils. Famotidine crosses intestinal epithelial cells via facilitated diffusion and passive diffusion, blocks paracellular cation transport, and increases intestinal transepithelial electrical resistance. Famotidine reduces serum levels of transaminases and alkaline phosphatase, exerts analgesic effects and gastric protective effects simultaneously. Famotidine can be used in studies related to COVID-19, liver injury and acute gastric ulcer.

PROTAC HPK1 Degrader-3 is an orally active, PROTAC degrader that selectively targets HPK1, with a DC₅₀ of 21.26 nM. PROTAC HPK1 Degrader-3 induces HPK1 degradation via the ubiquitin-proteasome system and forms a stable ternary complex with HPK1 and CRBN. It inhibits the SLP76 and NF-κB signaling pathways, enhances MAPK signal transduction, reverses the immunosuppressive factor-mediated inhibition of T cell cytokine secretion, and promotes the secretion of T cell immune cytokines. PROTAC HPK1 Degrader-3 suppresses tumor growth and enhances anti-PD-L1-mediated antitumor activity. It can be used in studies related to malignant tumors, such as colorectal cancer.

Pellitorine is a bioactive natural amide compound. Pellitorine can competitively antagonize the activation of TRPV1 by Capsaicin (HY-10448), thereby reducing pain signal transmission. Pellitorine improves cognitive dysfunction by upregulating the BDNF-ERK1/2-CREB and Nrf2-HO-1 pathways. Pellitorine exerts anti-inflammatory and anti-sepsis effects by inhibiting the release of high mobility group protein B1 (HMGB1) and the expression of RAGE/TLR4. Pellitorine exerts its antithrombotic effect by prolonging the clotting time, inhibiting the activity of clotting factors and thrombin. Pellitorine inhibits lipid peroxidation and resists ferroptosis by upregulating GPX4 and DHODH. Pellitorine kills Aedes aegypti mosquito larvae by inhibiting V-type H⁺-ATPase and aquaporin 4 (AaAQP4). Pellitorine exhibits anti-cancer activity (e.g., leukemia and breast cancer) and has inhibitory effects on certain bacteria.

Elaidic acid-d₉ is deuterium labeled Elaidic acid (HY-113016). Elaidic acid is an orally active trans fatty acid. Elaidic acid enhances the stemness of colorectal cancer cells by activating the Wnt/ERK1/2 pathway, thereby promoting cell proliferation, invasion and metastasis, and inhibiting apoptosis. Elaidic acid also inhibits the growth of Lactobacillus and alters the cell surface hydrophobicity of Lactobacillus. Elaidic acid reduces basal 2-deoxyglucose uptake in muscle cells and adipocytes. Elaidic acid can be used in research on colorectal cancer, insulin and other related areas.

Glutathione trisulfide (GSSSG) is an orally active, blood-brain barrier permeable neuroprotective agent. Glutathione trisulfide inactivates intracellular tyrosinase, regulates the expression of Cars2, Cbs, MITF and TYR, inhibits α-MSH (HY-P0252)-induced melanogenesis, and restores intracellular persulfide levels reduced by α-MSH. Glutathione trisulfide scavenges free radicals, quenches ROS, reduces Paclitaxel (HY-B0015)-induced superoxide production, upregulates the expression of antioxidant protein genes, and inhibits oxidative stress-induced cell death. Glutathione trisulfide promotes ERK1/2 activation, prevents NF-κB p65 activation, inhibits TAK1 phosphorylation, reduces pro-inflammatory cytokine expression, and blocks microglial activation. Glutathione trisulfide can be used in research related to dry age-related macular degeneration, inflammation-associated eye diseases, Alzheimer's disease, Parkinson's disease, etc.

Ganglioside GT1b (porcine) ammonium is a member of the ganglioside family. Ganglioside GT1b (porcine) ammonium acts as a protective signal against nerve injury-induced spinal synapse elimination. Ganglioside GT1b (porcine) ammonium induces HA synthesis and the phosphorylation of Akt/mTOR in orbital fibroblasts. Ganglioside GT1b (porcine) ammonium enhances porcine oocyte maturation and induces activation of EGFR and ERK1/2 signaling. Ganglioside GT1b (porcine) ammonium is a putative host cell receptor for the Merkel cell polyomavirus. Ganglioside GT1b (porcine) ammonium can be used for the researches of cancer, infection, immunology, endocrinology and neurological disease, such as Thyroid eye disease.

Q-Peptide is an angiopoietin-1 derived peptide (QHREDGS). Q-Peptide interacts with β1-integrin, binds to integrins on the surface of osteoblasts, and serves as an acyl donor substrate for Streptomyces mobaraensis transglutaminase. Q-Peptide activates Akt, MAPKp42/44, ILK, ERK1/2, and downregulates caspase-3/7. Q-Peptide inhibits cell apoptosis, enhances cell adhesion and migration, and promotes osteoblast differentiation, bone matrix deposition and mineralization. Q-Peptide can be used in studies related to myocardial infarction, bone regeneration, diabetic wound repair and human induced pluripotent stem cells.

ZEB85 is a human monoclonal antibody (mAb) targeting TrkB. ZEB85 activates TrkB and its downstream cascades, including the ERK, PLCγ, AKT, MAPK signaling pathways and cFOS expression, and enhances neuronal activity. ZEB85 prevents β-amyloid toxicity in cultured hippocampal neurons. ZEB85 is applicable to the research of Alzheimer's disease (AD).

Benzanthrone is an immunotoxic, pro-inflammatory Photosensitizer. Benzanthrone upregulates iNOS, COX-2 and inflammatory cytokines; activates ERK1/2, p38, JNK, AP-1 and NF-κB; inhibits Nrf2; and induces oxidative stress and DNA damage. Upon radiation exposure, Benzanthrone generates singlet oxygen and superoxide anion radicals, induces photohemolysis and lipid peroxidation, and alters the levels of skin xenobiotic enzymes. Benzanthrone exhibits differential genotoxicity in different cell lines. Benzanthrone possesses skin tumor-initiating and promoting activities. Benzanthrone can be used in skin tumor-related studies.

Propoxur is a reversible, competitive, orally active AChE inhibitor that can cross the blood-brain barrier. Propoxur inhibits AChE activity to induce neurotoxicity, while promoting MMP-2 expression and enhancing tumor cell migration and invasion by inducing intracellular ROS generation and activating the ERK/Nrf2 signaling pathway. On the one hand, Propoxur inhibits AChE, leading to acetylcholine accumulation and causing neurological dysfunction; on the other hand, it promotes Nrf2 nuclear translocation through ROS-dependent ERK1/2 phosphorylation, and upregulates MMP-2 and other invasion-related proteins. Propoxur is also a carbamate insecticide used to combat turf, forestry, and household pests.

Isoprocurcumenol is a guaiane type sesquiterpene, that can be isolated from Curcuma comosa. Isoprocurcumenol can activate EGFR signaling. Isoprocurcumenol increases the phosphorylation of ERK and AKT. Isoprocurcumenol promotes the proliferation of keratinocytes.

Sialorphin TFA is a neutral endopeptidase (NEP) and aminopeptidase N (APN) inhibitor that responds to androgen signals. Sialorphin TFA blocks the degradation of endogenous opioid peptides and interacts with μ-, δ-, κ-opioid receptors. Sialorphin TFA regulates the ERK/mTOR signaling pathway by inducing cell cycle arrest, enhancing ERK1/2 activity, and reducing the phosphorylation levels of mTOR, 4E-BP1, p70S6K; accordingly, Sialorphin TFA exhibits antiproliferative activity against colorectal cancer, glioma and prostate cancer cells without cytotoxicity. In addition, Sialorphin TFA also produces antinociceptive responses, regulates sexual behavior, relaxes corpus cavernosum smooth muscle, and alleviates experimental colitis. Sialorphin TFA is also a copper (II) ion-binding ligand. Sialorphin TFA has been used in mechanistic studies related to cancer, pain management and inflammatory bowel disease.