ERK Activator

Propoxur-d₃ is the deuterated form of Propoxur (HY-B0916). 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.

Zoniporide hydrochloride (CP-597396 hydrochloride) 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 hydrochloride 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 hydrochloride is applicable to research related to myocardial ischemia-reperfusion injury and heart graft ischemia-reperfusion injury.

αMβ2 integrin agonist-1 (Compound 8) is a highly selective αMβ2 integrin agonist with anti-inflammatory activity (EC₅₀=1.4 nM). αMβ2 integrin agonist-1 activates integrin-mediated cell adhesion and JNK/ERK signaling. αMβ2 integrin agonist-1 induces tumor-associated macrophage repolarization and enhances antitumor T-cell immune responses. αMβ2 integrin agonist-1 is promising for research of cancers and chronic inflammatory diseases (e.g., pancreatic cancer, rheumatoid arthritis).

MAPK-IN-3 (Compound 4a) is an anti-proliferative agent that shows particularly strong inhibitory effects on KYSE 30, HCT 116, and HGC 27, with IC₅₀ values of 0.57 μM, 3.27 μM, and 2.28 μM, respectively. MAPK-IN-3 blocks the cell cycle via a p53-dependent mechanism and induces cell apoptosis through a p53-independent mechanism. MAPK-IN-3 downregulates the expression of cell cycle-related proteins like Cyclin D1 and cyclin B1, upregulates pro-apoptotic proteins such as cleaved PARP, cleaved caspase-7, and cleaved caspase-9, and reduces the expression of anti-apoptotic proteins like Bcl-2. Additionally, MAPK-IN-3 increases the intracellular level of ROS in KYSE 30 cells and upregulates the expression of members of the MAPK signaling pathway associated with ROS, such as p-ERK, p-p38 and p-JNK.

HTL-9936 is an orally active partial agonist of muscarinic M1 receptor. HTL-9936 has an EC₅₀ of 32 nM for human M1 receptor and an EC₅₀ of 224 nM for human M4 receptor. HTL-9936 activates Gq/11 coupling, promotes inositol phosphate accumulation, ERK1/2 phosphorylation, β-arrestin recruitment and receptor internalization. HTL-9936 can be used in the research of Alzheimer's disease and schizophrenia.

(-)-Salcolin B (Tricin 4'-O-(threo-β-guaiacylglyceryl) ether) is an isomer of Salcolin B (HY-N16766) and anti-inflammatory agent. (-)-Salcolin B is isolable from Njavara. (-)-Salcolin B downregulates the activities of NF-κB and STAT3, reduces the expressions of iNOS and COX-2, activates the ERK signaling pathway, and inhibits LPS-induced NO and ROS production. (-)-Salcolin B induces Apoptosis. (-)-Salcolin B inhibits TPA (HY-18739)-induced ear edema. (-)-Salcolin B possesses antioxidant activity. (-)-Salcolin B can be used in research related to inflammatory diseases, colon adenocarcinoma, ovarian cancer and breast cancer.

Polygalasaponin XXXII is an orally active cognitive enhancer. Polygalasaponin XXXII promotes the phosphorylation of ERK, CREB, Synapsin I and TrkB. Polygalasaponin XXXII enhances basal synaptic transmission. Polygalasaponin XXXII attenuates Scopolamine (HY-N0296)-induced cognitive impairment and improves hippocampus-dependent learning and memory abilities. Polygalasaponin XXXII can be used in research related to cognitive dysfunction.

Brelgometon (ATH-1105) is an orally active HGF/MET positive modulator. Brelgometon activates downstream ERK and AKT cascades. Brelgometon reduces pro-inflammatory cytokine levels and extranuclear TDP-43 aggregation; it also upregulates EAAT2 expression and improves mitochondrial function. Brelgometon protects neurons from excitotoxicity, inflammation, oxidative stress and mitochondrial dysfunction; it also maintains neurite length, neuromuscular junction integrity and sciatic nerve function. Brelgometon alleviates motor function deterioration, maintains body weight and prolongs survival in ALS transgenic mice. Brelgometon is applicable to research related to amyotrophic lateral sclerosis.

DOR agonist 2 (Compound 3) is a Delta Opioid Receptor agonist. DOR agonist 2 can inhibit the expression of TNF-α, prevent NF-κB transport to the nucleus, and activate the G protein-mediated ERK1/2 pathway. DOR agonist 2 can be used in the study of neurodegenerative diseases.

Famotidine GMP (MK-208 GMP) is Famotidine (HY-B0377) produced in GMP guideline. Famotidine 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.

Calactin is a glycoside that can be isolated from Asclepias curassavica L.. Calactin activates caspase-3, caspase-8, caspase-9, and phosphorylates ERK. Calactin induces DNA damage, apoptosis, PARP cleavage, G2/M phase cell cycle arrest, shifts Bax/Bcl-2 expression, and shows anti-proliferation effects in leukemia cells. Calactin can be used for the research of leukemia.

Zoniporide dihydrochloride (CP-597396 dihydrochloride) 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 dihydrochloride 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 dihydrochloride is applicable to research related to myocardial ischemia-reperfusion injury and heart graft ischemia-reperfusion injury.

MA191 is a FLT3 PROTAC degrader. MA191 targets and degrades mutant FLT3-ITD protein by recruiting the VHL E3 ligase in a manner dependent on ubiquitination and BIM, thereby blocking aberrant downstream MAPK/STAT5 signaling pathways and inducing apoptosis. MA191 can be used in research related to acute myeloid leukemia.

Famotidine-¹³C₃ (MK-208-¹³C₃) is the ¹³C₃-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.

Cuspin-1 is a upregulator of Survival of Motor Neuron protein (SMN). Cuspin-1 upregulates SMN expression post-transcriptionally, and increases the phosphorylation of Erk. Cuspin-1 can be used for research of neurodegenerative disease, such as spinal muscular atrophy (SMA).

LQEQ-19 (mouse, rat) is a VGF derived peptide that exerts neuroprotective effects. LQEQ-19 (mouse, rat) activates the PI3K/Akt and MEK/ERK signaling pathways by promoting phosphorylation of Akt and ERK1/2. LQEQ-19 (mouse, rat) is commonly used in the study of neurological conditions.

Aminoguanidine-¹³C,¹⁵N₂ (Pimagedine-¹³C,¹⁵N₂) hemisulfate is the ¹³C,¹⁵N₂-labeled Aminoguanidine hemisulfate (HY-W020772). Aminoguanidine hemisulfate is an inhibitor of diamine oxidase (DAO) and nitric oxide synthase (NOS). Aminoguanidine hemisulfate can reduce the formation of advanced glycation end products (AGEs). Aminoguanidine hemisulfate has a dose-dependent inhibitory effect on Doxorubicin (HY-15142)-induced cell apoptosis. Aminoguanidine hemisulfate has antioxidant properties. Aminoguanidine hemisulfate can be used in the research of diabetic nephropathy.

Pizotifen hydrochloride (Pizotyline hydrochloride) is a 5-HT₂ receptor antagonist. Pizotifen hydrochloride inhibits the Wnt/β-catenin-EMT signaling pathway and induces mitochondria-mediated Apoptosis. Pizotifen hydrochloride causes transient ERK1/2 phosphorylation and restores ATP. Pizotifen hydrochloride blocks Serotonin (HY-B1473A)-mediated platelet activation, inhibits Serotonin-enhanced ADP-induced platelet aggregation, and prolongs carotid artery occlusion and tail bleeding time. Pizotifen hydrochloride exhibits anticancer activity against gastric cancer and colon cancer. Pizotifen hydrochloride exerts neuroprotective effects in the striatum of R6/2 mice. Pizotifen hydrochloride can be used for research on gastric cancer, colon cancer, Huntington's disease, metastasis, and thromboembolic diseases.

Famotidine-d₄ (MK-208-d₄) is the deuterated-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.

Cyclazosin is an α₁D-adrenergic receptor antagonist and a partial agonist of CXCR4/ACKR3. The pKi values of Cyclazosin for cloned human α₁D, α₁B and α₁A adrenergic receptors are 9.28, 9.23 and 8.18, respectively. Cyclazosin induces β-arrestin recruitment in CXCR4 and ACKR3 with EC50 values of 16 μM and 10 μM, respectively, stimulates ERK1/2 phosphorylation, and induces receptor internalization. Cyclazosin potently inhibits CXCL12-induced chemotaxis of primary human aortic vascular smooth muscle cells. Cyclazosin alters MDMA-induced thermoregulatory responses in mice, converting monophasic hyperthermia to a biphasic pattern without affecting resting core body temperature. Cyclazosin can be used for diseases related to tumor metastasis, MDMA-induced hyperthermia and vasoconstriction.