ERK Activator

Elaidic acid-d₁₇ 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.

α-Amyrin (Standard) is a pentacyclic triterpenoid compound with oral activity. α-Amyrin (Standard) activates the ERK and GSK-3β signaling pathways. α-Amyrin (Standard) can inhibit cancer cells proliferation and induce apoptosis. α-Amyrin (Standard) shows anti-bacterial and anti-inflammation activity. α-Amyrin (Standard) can reduce blood glucose level. α-Amyrin (Standard) can be used for the researches of cancer, infection, inflammation, metabolic disease and neurological disease, such as breast cancer, Streptococcus oralis infection, skin inflammation and diabetes.

Ferroptosis inducer-7 is an orally active and selective ferroptosis inducer via inositol 1,4,5-trisphosphate receptor (IP₃R)/calcium release-activated calcium channel protein (ORAI). Ferroptosis inducer-7 exhibits a notable effect in alleviating anemia symptoms, suppressing bone marrow CTLs activation, and improving hematopoietic function in immune-mediated bone marrow failure. Ferroptosis inducer-7 can be studied in research for aplastic anemia.

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.

Rapastinel (GLYX-13) acetate is a potent NMDAR modulator capable of crossing the blood-brain barrier, and it exhibits extremely high affinity for human NMDAR (EC₅₀=0.0017-9.9 nM). Rapastinel acetate enhances ERK signaling and activates the mTOR pathway, thereby upregulating the expression of BDNF and VGF, and inducing significant neuroplastic changes such as enhanced LTP and increased mature dendritic spine density in the hippocampus. Rapastinel acetate moderately elevates the efflux of dopamine, norepinephrine and 5-HT in the prefrontal cortex, and uniquely avoids side effects of traditional antidepressants such as dissociation, addiction or sedation. Rapastinel acetate is applicable to the research of major depressive disorder and hepatocellular carcinoma.

NS-417 free base is an ERK1, ERK2, and Akt kinase activator with neuroprotective, neurite outgrowth potentiating, and dopaminergic cell population enhancing activity. NS-417 free base enhances activation of ERK1, ERK2, and Akt kinase via growth factor stimulation. NS-417 free base rescues cells from growth factor withdrawal-induced death, stimulates neurite outgrowth, increases tyrosine hydroxylase-positive cell counts, and displays neurotrophic-like activity in in vitro models. NS-417 free base can be used for the research of parkinson’s disease.

Dimethoxycurcumin-d₆ (DiMC-d₆; CHC 004-d₆; Di-O-methylcurcumin-d₆) is the deuterated-labeled Dimethoxycurcumin (HY-100977). Dimethoxycurcumin (DiMC) is a curcuminoid compound found in Curcuma longa. Dimethoxycurcumin is also an orally active thioredoxin reductase inhibitor (IC₅₀ = 5.4 μM) and androgen receptor antagonist. Dimethoxycurcumin inhibits thioredoxin reductase, leading to oxidized thioredoxin accumulation, ROS production, DNA damage, glutathione depletion, mitochondrial membrane potential decrease, ATP depletion, S phase arrest, and apoptosis. Dimethoxycurcumin inhibits NF-κB, NADPH oxidase subunits, ATP synthase subunits, CDK4, cyclin-D1, FASN, ACC, and the IRS2-PI3K-Akt pathway, while activating AMPK, ERK, and JNK. Dimethoxycurcumin can be used for research on cancer, arsenic-induced hepatotoxicity, and tuberculosis.

BR103354 is an orally active, selective fibroblast activation protein (FAP) inhibitor with an IC₅₀ value of 14 nM against hFAP. BR103354 restores the levels of phosphorylated ERK and Glut1 that are reduced by co-treatment with hFGF21 and FAP, decreases non-fasting blood glucose concentrations, improves glucose tolerance, and reduces hepatic triglyceride content. BR103354 ameliorates hepatic steatosis and hepatic fibrosis. BR103354 can be used in the research of type 2 diabetes and non-alcoholic steatohepatitis.

Pyridoxal 5'-​phosphate (monohydrate) (Standard) is the analytical standard of Pyridoxal 5'-​phosphate (monohydrate). This product is intended for research and analytical applications. Pyridoxal 5'-phosphate monohydrate, the active form of vitamin B6, is an essential cofactor for multiple enzymes, including aromatic l-amino acid decarboxylase that catalyzes the final stage in the production of the neurotransmitters dopamine and serotonin. Pyridoxal 5'-phosphate monohydrate is the most important coenzyme variant in the process of vitamin B6 intracellular phosphorylation and is interconvertible with other variants, including pyridoxine 5′‐phosphate (PNP) and pyridoxamine 5′-phosphate (PMP).

M1/M4 muscarinic agonist 4 is a dual-site muscarinic acetylcholine receptor ligand with potent agonistic activity at M1/M4 muscarinic acetylcholine receptors. M1/M4 muscarinic agonist 4 activates M1R to induce phosphorylation of ERK1/2, and activates M4R to induce GαoB protein activation as well as ERK1/2 phosphorylation. M1/M4 muscarinic agonist 4 exhibits higher binding affinity for M4R than for other muscarinic receptors, while its binding affinity for the W435A mutant M4R is reduced. M1/M4 muscarinic agonist 4 can be used in the research of schizophrenia.

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

Endothelin-1 (1-31) (Human) acetate is a potent vasoconstrictor and hypertensive agent. Endothelin-1 (1-31) (Human) acetate is derived from the selective hydrolysis of big ET-1 by chymase.

UFP-512 is a selective and potent σ-opioid receptor (DOP receptor) peptidic agonist with antidepressant- and anxiolytic-like effects. UFP-512 exhibits as a potent agonist on adenylyl cyclase inhibition and Erk1/2 activation. UFP-512 induces phosphorylation of DOP receptors on Ser³⁶³ with a low desensitization of the cAMP pathway. UFP-512 is promising for research of mood disorders.

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.