ERK Activator

Sialorphin is a neutral endopeptidase (NEP) and aminopeptidase N (APN) inhibitor that responds to androgen signals. Sialorphin blocks the degradation of endogenous opioid peptides and interacts with μ-, δ-, κ-opioid receptors. Sialorphin 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 exhibits antiproliferative activity against colorectal cancer, glioma and prostate cancer cells without cytotoxicity. In addition, Sialorphin also produces antinociceptive responses, regulates sexual behavior, relaxes corpus cavernosum smooth muscle, and alleviates experimental colitis. Sialorphin is also a copper (II) ion-binding ligand. Sialorphin has been used in mechanistic studies related to cancer, pain management and inflammatory bowel disease.

SMU-L11-R is a selective TLR7 agonist with an EC₅₀ of 0.012 μM for human TLR7. SMU-L11-R specifically activates TLR7, recruits  MyD88, and triggers MAPK/NF-κB pathways, leading to TNF-α/IL-1β/IL-6 secretion in both mouse and human peripheral blood mononuclear cells. SMU-L11-R promotes M1-like macrophage polarization. SMU-L11-R exhibits excellent synergistic anti-tumor effects with PD-L1 inhibitors by upregulating CD8⁺T cells. SMU-L11-R shows potential in colorectal cancer studies.

VSLRGDTRG is a synthetic peptide containing the RGD motif from cadherin 17 (CDH17), which binds to α2β1 integrin and activates its signaling pathway. VSLRGDTRG promotes the high-affinity conformational change of β1 integrin through the RGD motif, enhancing cell adhesion and phosphorylation of FAK and ERK1/2, thereby driving tumor proliferation and metastasis. VSLRGDTRG can be used in research on cancers expressing CDH17, such as colon cancer and pancreatic cancer.

Breceptin (B 9870) is an antagonist of the bradykinin B₁/B₂ receptor (B₁/B₂R). Breceptin exhibits an irreversible antagonist effect on B₂R, inhibiting the vasodilation induced by Bradykinin (HY-P0206) in the rabbit carotid vein contraction experiment. B-9870 shows partial agonist properties in HEK 293 cells with high expression of B₂R, and can activate ERK1/2 phosphorylation, calcium ion mobilization, arachidonic acid release, and receptor internalization. Breceptin can be used in research to inhibit breast cancer and non-small cell lung cancer.

Propoxue (Standard) is the analytical standard of Propoxue (HY-B0916). This product is intended for research and analytical applications. 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.

SHP1‑IN‑2 is a selective and orally active SHP1 inhibitor. SHP1‑IN‑2 covalently binds to Cys480 of SHP1. SHP1‑IN‑2 elicits potent antitumor immunity and suppresses syngeneic tumor growth. SHP1‑IN‑2 blocks tumor progression in a svngeneic cancer model by activating natural killer cells and cytotoxic CD8^＋ T cells, along with reduced T cel l. SHP1‑IN‑2 can be used for cancer‑related research.

Cudraflavone B is a prenylated flavonoid with anti-inflammatory and anti-tumor properties. Cudraflavone B is also a dual inhibitor of COX-1 and COX-2. Cudraflavone B blocks the translocation of nuclear factor κB (NF-κB) from the cytoplasm to the nucleus in macrophages. Thus, Cudraflavone B inhibits tumor necrosis factor α (TNFα) gene expression and secretion. Cudraflavone B also triggers the mitochondrial apoptotic pathway, activates NF-κB, the MAPK p38, and ERK, and induced the expression of SIRT1. Thus Cudraflavone B inhibits the growth of human oral squamous cell carcinoma cells.

Dinitramine is a herbicide. Dinitramine activates the Erk/P38/JNK/MAPK pathway and inactivates the PI3k/Akt pathway in testicular cells. Dinitramine induces endoplasmic reticulum stress, dysregulation of calcium homeostasis in the cytoplasm and mitochondria, apoptosis, and downregulated expression of cell cycle genes in testicular cells. Dinitramine reduces the viability and proliferation capacity of testicular cells, and inhibits cell division by suppressing the synthesis of tubulin. Dinitramine induces abnormal heart development, inhibited angiogenesis, inflammatory responses, apoptosis, and impaired embryonic growth in zebrafish embryos.

Famotidine-¹³C,d₃ (MK-208-¹³C,d₃) is the deuterated, ¹³C-labeled Famotidine (HY-B0377). 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.

Propoxur-d₇ is the deuterium labeled Propoxur. 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.

MRS2693 trisodium is a selective P2Y6 agonist with an EC₅₀ value of 0.015 μM. MRS2693 trisodium can reduce the activation of NF-kappaB and activate the ERK1/2 pathway, and has a cytoprotective effect on mouse hindlimb skeletal muscle ischemia-reperfusion injury model.

Withanolide B (Standard) is the analytical standard of Withanolide B. This product is intended for research and analytical applications. Withanolide B is an active component of W. somnifera Dunal. Withanolide B promotes osteogenic differentiation of hBMSCs via ERK1/2 and Wnt/β-catenin signaling pathways. Withanolide B exhibits neuroprotective, anti-arthritic, anti-aging and anti-cancer effects.

Geranylgeranyl pyrophosphate is a type of isoprenoid metabolic intermediate, mainly synthesized through the mevalonate pathway. Geranylgeranyl pyrophosphate is a key precursor in various biological synthesis processes, especially as a necessary substrate for post-translational modification of proteins - geranylgeranyl phosphorylation. Geranylgeranyl pyrophosphate regulates various cellular processes and disease progression through protein geranylgeranyl phosphorylation, such as activating the YAP signaling pathway, promoting cell proliferation and inhibiting apoptosis; promoting IL-2 production and STAT5 phosphorylation; and influencing metabolic homeostasis and cancer, etc.

DSO-5a is a potent, selective, orally active BB₃ agonist. DSO-5a is a representative DMAKO-00 derivative compound. DSO-5a upregulates ppar-γ activity through BB₃ and activates ERK1/2 phosphorylation. DSO-5a can be used in diabetes-related research.

Zoniporide (Standard) (CP-597396 (Standard)) is the analytical standard of Zoniporide (HY-105064). This product is intended for research and analytical applications. Zoniporide (CP-597396) is a selective Na⁺/H⁺ exchanger subtype 1 (NHE1) inhibitor with cardioprotective activity, with IC₅₀ values of 67 nM and 73 nM against rat NHE1. Zoniporide reduces intracellular Na⁺ and Ca²⁺ overload, preserves mitochondrial integrity, activates pro-survival ERK1/2 and STAT3 signaling pathways, reduces necrosis and apoptosis, and decreases neutrophil aggregation. Zoniporide is applicable to research related to myocardial ischemia-reperfusion injury and heart graft ischemia-reperfusion injury.

Fenoprofen (LILLY-53858 (Standard)) (Standard) Calcium hydrate is the analytical standard of Fenoprofen Calcium hydrate (HY-B0288B). This product is intended for research and analytical applications. Fenoprofen is a nonsteroidal anti-inflammatory agent (NSAID) and inhibits cyclooxygenase (COX). Fenoprofen is a melanocortin receptors (MCRs) positive allosteric modulator (PAM). Fenoprofen also increases ERK1/2 activation in HEK293T cells. Fenoprofen has anti-arthritic activities and can be used for the study of rheumatoid arthritis and osteoarthritis.

Famotidine hydrochloride (MK-208 hydrochloride) 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 hydrochloride inhibits TLR3-mediated inflammatory pathways, and reduces the expression of various inflammatory mediators and interferon-related genes. Famotidine hydrochloride 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 hydrochloride crosses intestinal epithelial cells via facilitated diffusion and passive diffusion, blocks paracellular cation transport, and increases intestinal transepithelial electrical resistance. Famotidine hydrochloride reduces serum levels of transaminases and alkaline phosphatase, exerts analgesic effects and gastric protective effects simultaneously. Famotidine hydrochloride can be used in studies related to COVID-19, liver injury and acute gastric ulcer.

Simetryn (Standard) is the analytical standard of Simetryn (HY-B1853). This product is intended for research and analytical applications. Simetryn is a triazine herbicide that exerts teratogenicity. Simetryn inhibits photosynthesis by blocking electron transfer in the chloroplast photosystem II and activates the MEK/Erk signaling pathway. Simetryn triggers vascular and developmental abnormalities in zebrafish and tadpoles, suppresses proliferation, enhances apoptosis, and induces malformations. Simetryn serves as a tool to establish a zebrafish model for studying arteriovenous malformations and related pathogenesis. Simetryn controls paddy weeds and can be used for research on developmental and vascular disorders.

Recoflavone (Standard) is the analytical standard of Recoflavone (HY-106449). This product is intended for research and analytical applications. Recoflavone (DA-6034 (free acid)), a synthetic derivative of the flavonoid Eupatilin (HY-N0783), is orally active. Recoflavone can inhibit the NF-κB pathway and induce [Ca(2+)]i increase in epithelial cells. Recoflavone exhibits activities such as anti-inflammation, anti-tumor effects, protection of gastric and intestinal mucosa, and promotion of secretion in the ocular surface and salivary glands. Recoflavone can be used for the research of diseases such as dry eye, gastric injury, and intestinal injury.

Varenicline (Tartrate) (Standard) is the analytical standard of Varenicline (Tartrate). This product is intended for research and analytical applications. Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC₅₀ = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α6β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation.