p38 MAPK Activator

Histamine-¹⁵N₃ is the ¹⁵N₃-labeled Histamine (HY-B1204). Histamine is the agonist for histamine receptor and a vasodilator. Histamine is an organic nitrogen compound that participates in local immune responses, regulates intestinal physiological functions, and acts as a neurotransmitter. Histamine affects p38 MAPK/Akt signaling pathway, exhibits antitumor, antioxidant and anti-inflammatory activities. Histamine can be used in the research of acute myeloid leukemia, malignant melanoma, and renal cell carcinoma.

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.

Semaglutide sodium is a long-acting, selective, competitive GLP-1R agonist that can penetrate the blood-brain barrier. After activating GLP-1R, Semaglutide sodium promotes insulin secretion, inhibits gastric emptying and appetite, and at the same time enhances autophagy, inhibits oxidative stress and apoptosis. Semaglutide sodium also regulates mitochondrial function and lipid metabolism (such as reducing de novo lipogenesis in the liver). Semaglutide sodium has activities such as lowering blood sugar, reducing weight, neuroprotection (such as improving motor function in Parkinson's disease models, reducing α-synuclein aggregation) and improving hepatic steatosis. Semaglutide sodium can be used for the study of neurodegenerative diseases and liver diseases such as type 2 diabetes, obesity, Parkinson's disease, metabolic associated fatty liver disease (MASLD), and cancer.

Platycodin D (Standard) is the analytical standard of Platycodin D. This product is intended for research and analytical applications. Platycodin D is a saponin isolated from Platycodon grandiflorus, acts as an activator of AMPKα, with anti-obesity property. WNT/β-catenin pathway mediates the anti-adipogenic effect of platycodin D.

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.

Picolinafen is a pyridine-class herbicide that acts as a phytoene desaturase (PDS) inhibitor. Picolinafen effectively controls broadleaf weeds and disrupts carotenoid biosynthesis. Picolinafen exhibits cytotoxicity to porcine trophectoderm (pTr) and luminal epithelial (pLE) cells. Picolinafen induces (ROS accumulation, calcium depletion, and activates (MAPK and PI3K signaling pathways, leading to decreased cell viability, increased apoptosis, impaired migration, and altered expression of implantation-related genes. Picolinafen has an LD₅₀ value of 2.7 mg/kg in mammals and 7 μg/L in fish. Picolinafen exhibits toxic effects during zebrafish embryogenesis^[1][2].

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.

MRS2690 is a selective P2Y14 receptor agonist. MRS2690 inhibits adenylyl cyclase activity, thereby reducing intracellular cAMP levels and mediating concentration-dependent vasoconstriction of porcine coronary arteries. MRS2690 induces intracellular calcium mobilization, activates P38 and stimulates [³⁵S]GTPγS binding to RBL-2H3 cell membranes. MRS2690 enhances antigen (NP-BSA)-, C3a-induced β-hexosaminidase (β-Hex) release. MRS2690can be used for ischemic heart disease.

(R)-Bromoenol lactone-d₇ ((R,E)-Bromoenol lactone-d₇) is the deuterated-labeled (R)-Bromoenol lactone (HY-117068). (R)-Bromoenol lactone ((R,E)-Bromoenol lactone) is an isomer of Bromoenol lactone (HY-107411). (R)-Bromoenol lactone acts as a selective inhibitor of microsomal calcium-independent phospholipase A2γ (iPLA2γ). (R)-Bromoenol lactone induces mild activation of p38 mitogen-activated protein kinase in prostate cancer cells, resulting in slight increases in the expressions of phosphorylated p53, total p53 and p21. (R)-Bromoenol lactone is applicable to prostate cancer-related research.

PROTAC Bcl-xL degrader-4 is a Bcl-xL PROTAC degrader. PROTAC Bcl-xL degrader-4 exhibits cytotoxicity against hepatocellular carcinoma cells, inhibits their migration and colony formation, and shows low cytotoxicity toward normal cells. PROTAC Bcl-xL degrader-4 induces apoptosis by reducing mitochondrial membrane potential and activating the MAPK signaling pathway. PROTAC Bcl-xL degrader-4 significantly suppresses tumor growth in xenograft tumor mouse models. PROTAC Bcl-xL degrader-4 can be used in hepatocellular carcinoma-related research.

Pancracine is an alkaloid. Pancracine upregulates p27, phosphorylated p38 MAPK and phosphorylated p53, while downregulating phosphorylated Akt and phosphorylated Rb. Pancracine induces G₁ cell cycle arrest and Apoptosis in cells. Pancracine inhibits the replication of pseudotyped HIV-1 and Dengue virus. Pancracine can be used in research related to lung adenocarcinoma, acute lymphoblastic leukemia, cutaneous epidermoid carcinoma, human immunodeficiency virus infection and dengue virus infection.

(±)-Iroxanadine (BRX 005; BRX 235), a vasculoprotector, is a p38 kinase and HSP protein activator. (±)-Iroxanadine has the potential for atherosclerosis and vascular diseases research.

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.

ML-7 is a selective and highly specific myosin light chain kinase (MLCK) inhibitor that acts as a trabecular meshwork (TM) relaxant. ML-7 enhances Quinocetone (HY-123581)-induced phosphorylation of ERK, p38 MAPK and JNK, attenuates Akt activation, and promotes apoptosis of hepatocellular carcinoma cells. ML-7 reduces Th2 cytokine secretion by inhibiting MLCK, while alleviating smooth muscle hyperplasia and collagen deposition. As a non-antibiotic adjuvant, ML-7 restores the sensitivity of drug-resistant bacteria to Tigecycline (HY-B0117). ML-7 can be used in research related to glaucoma, hepatocellular carcinoma, asthma, and Klebsiella pneumoniae infection.

Cyproheptadine (Standard) is the analytical standard of Cyproheptadine (HY-B1622). This product is intended for research and analytical applications. Cyproheptadine acts as a p38 MAP kinase activator, CHK2 activator, histamine H1 receptor inhibitor and serotonin receptor inhibitor. Cyproheptadine mediates cell cycle arrest via G1 phase arrest, G1/S transition arrest, G0/G1 phase arrest, reduced expression of cyclins D1/D2/D3, upregulated expression of HBP1, p16, p21, p27, and decreased phosphorylation of retinoblastoma protein. Cyproheptadine induces Apoptosis by increasing PARP and cleaved PARP, as well as activating the mitochondrial caspase pathway. Cyproheptadine inhibits tumor growth with extremely low toxicity to normal cells. Cyproheptadine can be used in research related to hepatocellular carcinoma, multiple myeloma and acute myeloid leukemia.

Phenylhydroquinone (PHQ) is an orally active thymic atrophy inducer which can up-regulate apoptosis through activation of p53. PHQ can be used for research of thymic atrophy.

Isosalvianolic acid C is a naturally derived phenolic compound that acts as a signal modulator, antioxidant, and enzyme inhibitor. Isosalvianolic acid C induces the phosphorylation of PLC-γ, IP3R, PKC, and P38, triggering Ca²⁺ mobilization, degranulation, and chemokine release. Isosalvianolic acid C activates MRGPRX2 and its murine homolog MrgprB2, leading to pseudo-allergic reactions in vivo. Isosalvianolic acid C inhibits Cu²⁺-induced LDL peroxidation. Isosalvianolic acid C can be used in studies related to pseudo-allergy, diabetes, and atherosclerosis.

Pratol (7-Hydroxy-4'-methoxyflavone) is an NF-κB inhibitor. Pratol also inhibits NO, PGE₂, TNF-α, IL-1β, and IL-6 production. Pratol increases the phosphorylation of p38 MAPK, JNK, and ERK, decreases AKT phosphorylation, and upregulates MITF, tyrosinase, TRP-1, and TRP-2 through a PKA-dependent signaling pathway. Pratol reduces iNOS and COX-2 protein expression, inhibits p65 phosphorylation, and protects IκBα from degradation, thereby inhibiting NF-κB nuclear translocation. Pratol can be used in research on hypopigmentary disorders, inflammatory diseases, cervical cancer, and colon cancer.

O6-Benzylguanine sodium is an orally active, blood-brain barrier-penetrant inhibitor of O⁶-methylguanine-DNA methyltransferase (MGMT/AGT). O6-Benzylguanine sodium modulates p53 and its downstream p21 and cyclins to induce cell cycle arrest and apoptosis, and on the other hand activates mTORC1/MAPK and other signaling pathways to induce cellular senescence by inhibiting intracellular MGMT. O6-Benzylguanine sodium is used in research related to various tumors, cellular senescence, and vascular smooth muscle dysfunction.

Muramyl dipeptide (Standard) is the analytical standard of Muramyl dipeptide (HY-127090). This product is intended for research and analytical applications. Muramyl dipeptide (MDP) is a synthetic immunoreactive peptide, consisting of N-acetyl muramic acid attached to a short amino acid chain of L-Ala-D-isoGln. Muramyl dipeptide is an inducer of bone formation through induction of Runx2. Muramyl dipeptide directly enhances osteoblast differentiation by up-regulating Runx2 gene expression through MAPK pathways. Muramyl dipeptide is a NLRP1 agonist.