ERK1 Activator

Yoda 1 is a potent and selective Piezo1 agonist. Yoda 1 activates purified Piezo1 channels. Yoda 1 potently inhibits macropinocytosis induced by epidermal growth factor (EGF). Yoda 1 enhances Ca²⁺ influx followed by activation of the calcium-activated potassium channel KCa3.1 and inhibition of Rac1 activation.

β-Glycerophosphate disodium salt pentahydrate is a bioactive endogenous metabolite and a phosphatase inhibitor. β-Glycerophosphate disodium salt pentahydrate plays an important role in inducing and maintaining osteoblast differentiation, mineral metabolism and signal transduction, and can be used as a drug carrier to form heat-sensitive hydrogels. β-Glycerophosphate disodium salt hydrate accelerates the calcification of vascular smooth muscle cells.

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.

Honokiol is a bioactive, biphenolic phytochemical that possesses potent antioxidative, anti-inflammatory, antiangiogenic, and anticancer activities by targeting a variety of signaling molecules. It inhibits the activation of Akt. Honokiol can readily cross the blood brain barrier.

β-Glycerophosphate disodium salt pentahydrate is a bioactive endogenous metabolite and a phosphatase inhibitor. β-Glycerophosphate disodium salt pentahydrate plays an important role in inducing and maintaining osteoblast differentiation, mineral metabolism and signal transduction, and can be used as a drug carrier to form heat-sensitive hydrogels. β-Glycerophosphate disodium salt hydrate accelerates the calcification of vascular smooth muscle cells.

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.

Urocortin II, human is a selective endogenous peptide agonist of type-2 corticotropin-releasing factor (CRF2) receptor. Urocortin II, human has an effect of promoting satiet and neuroprotective effect. Urocortin II, human also has bactericidal, antiparasitic and pro-inflammation activity. Urocortin II, human can activate NF-κB pathway and ERK1/2 MAP kinase. Urocortin II, human can reduce pulmonary arterial hypertension and shows cardiac protection effect. Urocortin II, human can be used for the researches of infection, inflammation, metabolic, neurological and cardiovascular disease.

Leucic acid (α-Hydroxyisocaproic acid) is an orally active end-product of the microbial metabolism of leucine. Leucic acid can bind to HCAR2, alters AMPK and ERK1/2 phosphorylation status, suppresses lipid synthesis, promotes catabolism, reduces adiposity, enhances lean mass and exercise capacity. Leucic acid suppresses pro-inflammatory cytokine secretion, inflammation-related gene mRNA expression. Leucic acid decreases basal protein synthesis, attenuates myotube atrophy. Leucic acid can be used for the research of obesity.

H-Ile-Lys-Val-Ala-Val-OH is one of the most potent active sites of laminin-1. H-Ile-Lys-Val-Ala-Val-OH promotes cell adhesion, neurite outgrowth, and tumor growth. H-Ile-Lys-Val-Ala-Val-OH stimulates BMMSC population growth and proliferation by activating MAPK/ERK1/2 and PI3K/Akt signalling pathways.

Ganglioside GM1 is a type of glycosphingolipid, mainly found on the cell membranes of the central nervous system of vertebrates. Ganglioside GM1 exerts neuroprotective effects by reducing excessive activation of NMDAR, activating TrkA and ERK1/2, and inhibiting oxidative stress and cell apoptosis and autophagy. Ganglioside GM1 can be used in the research of diseases such as traumatic brain injury, Parkinson's disease, Alzheimer's disease, and Huntington's disease.

Paeonolide, found in Paeonia suffruticosa, is an ERK1/2 activator. Paeonolide promotes early and late osteoblast differentiation, stimulates pre-osteoblast transmigration, and activates the BMP-Smad1/5/8, Wnt-β-catenin, JNK and p38 pathways. Paeonolide can be used for the research of osteoporosis, periodontitis.

CKLF1-C27, a C-terminal peptide of CKLF1, binds to CCR4 receptor and activates ERK1/2 pathway. CKLF1-C27 can abrogate the effect of CKLF1 on cells by competing for CCR4 receptor. CKLF1-C27 shows great effect on promoting proliferation on HUVECs. CKLF1-C27 has the potential for psoriasis research.

β-Neo-Endorphin is an endogenous opioid peptide. β-Neo-Endorphin is a hypothalamic “big” Leu-enkephalin of porcine origin. β-Neo-Endorphin shows activation of the Erk1/2, MMP-2 and MMP-9.

4-Methylbenzylidene camphor (4-MBC) is an endocrine disrupter that produces estrogen-like effects. 4-Methylbenzylidene camphor decreases the proliferation of human trophoblast cells and induces apoptosis. 4-Methylbenzylidene camphor activates PI3K/AKT and ERK1/2 signaling pathways and elevates intracellular ROS production. 4-Methylbenzylidene camphor is a ultraviolet (UV) filter and may hamper normal placental formation during early pregnancy.

FZ1 peptide is a cyclic heptapeptide and also an integrin αvβ3 agonist. FZ1 peptide activates the FAK/PI3K-AKT/ERK pathway and upregulates VEGFC to promote angiogenesis. FZ1 peptide exhibits antibacterial activity in extracts of HA-c-FZ1 hydrogel; it inhibits LPS-induced proinflammatory cytokine secretion in RAW264.7 macrophages; it reduces H₂O₂-induced ROS levels; it increases the healing rate of scratch wounds. FZ1 peptide can be used in studies related to diabetic skin wounds.

TCB-32 (Compound I-1) hydrochloride is a FGFR1 agonist with an EC₅₀ of 0.88  μM. TCB-32 hydrochloride significantly increases cell proliferation through activating FGFR1 signaling pathway as bFGF and its downstream ERK1/2 with excellent thermal stability. TCB-32 hydrochloride can replace bFGF in serum-free cell culture media. TCB-32 hydrochloride can be used for tissue repair and wound healing related diseases like psoriasis and eczema research.

Urocortin II, human acetate is a selective endogenous peptide agonist of type-2 corticotropin-releasing factor (CRF2) receptor. Urocortin II, human acetate has an effect of promoting satiet and neuroprotective effect. Urocortin II, human acetate also has bactericidal, antiparasitic and pro-inflammation activity. Urocortin II, human acetate can activate NF-κB pathway and ERK1/2 MAP kinase. Urocortin II, human acetate can reduce pulmonary arterial hypertension and shows cardiac protection effect. Urocortin II, human acetate can be used for the researches of infection, inflammation, metabolic, neurological and cardiovascular disease.

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

Cathepsin G is a pH-dependent serine protease. Cathepsin G hydrolyzes diverse synthetic and protein substrates and remodels extracellular matrix. Cathepsin G exerts immunomodulatory effects via recruiting phagocytes, enhancing T cell motility, activating ERK1/2 and p38 MAPK signaling, and mediating PKCζ membrane translocation. Cathepsin G regulates inflammatory responses by cleaving inflammatory mediators. Cathepsin G participates in vascular regulation by converting angiotensin I to angiotensin II. Cathepsin G induces PAR4-dependent platelet activation, facilitates platelet-neutrophil aggregation, and mediates VITT-related NETosis, thrombus formation. Cathepsin G can be used for the research of immune thrombotic thrombocytopenia, cardiovascular disease, and select autoimmune and inflammatory diseases.

Satratoxin H is a toxic metabolite of Stachybotrys atra. Satratoxin H induces caspase-3 and PARP cleavage via p38 MAPK and JNK pathways, stimulates JNK, ERK, and p38 MAPK phosphorylation, and activates JNK and p38 MAPK in a glutathione-sensitive manner. Satratoxin H induces DNA double-stranded breaks, apoptotic body formation, intracellular reactive oxygen species generation, and endoplasmic reticulum stress via ATF6, PERK, and IRE1 pathways. Satratoxin H can be used for the research of central nervous system disorders and melanoma.