1. Signaling Pathways
  2. MAPK/ERK Pathway
  3. p38 MAPK

p38 MAPK

The p38 MAPK family consists of highly conserved proline-directed serine-threonine protein kinases that are activated in response to a number many growth factors, cytokines, and chemotactic substances, such as vascular endothelial growth factor (VEGF), fibroblast growth factor (FGF), PDGF, TNF, interleukins, lipopolysaccharide (LPS) and formyl-methionyl-leucyl-phenylalanine (fMLP). It is well known that p38 is involved in inflammation, apoptosis, cardiomyocyte hypertrophy and cell differentiation.

The p38 MAPK family is composed of four proteins: p38α (encoded by the gene Mapk14), p38β (Mapk11), p38γ (Mapk12), and p38δ (Mapk13). Their coding genes have a distinct tissue distribution and they appear differentially expressed, being Mapk14 the most highly expressed. p38 MAPKs are substrates for three MAP2K (MKK6, MKK3, and MKK4). The contribution of each of these MAP2K to p38 MAPKs activation depends on the stimulus and the cell type. The MAP3Ks that lead to p38 MAPKs activation are ASK1, DLK1, TAK1, TAO1, TAO2, TPL2, MLK3, MEKK3, MEKK4, and ZAK1.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-12511
    SKF-86002
    Inhibitor 99.91%
    SKF-86002 is an orally active p38 MAPK inhibitor, with anti-inflammatory, anti-arthritic and analgesic activities. SKF-86002 inhibits lipopolysaccharide (LPS)-stimulate human monocyte IL-1 and TNF-α production (IC50 = 1 μM). SKF-86002 inhibits lipoxygenase- and cyclooxygenase-mediated metabolism of arachidonic acid.
    SKF-86002
  • HY-10261B
    (E/Z)-Afatinib
    Inhibitor 99.98%
    (E/Z)-Afatinib ((E/Z)-BIBW 2992) is the mixture of (E)-Afatinib and (Z)-Afatinib. Afatinib (HY-10261) is an irreversible inhibitor of EGFR, by irreversibly binding to their ATP binding site to block activation of EGFR, HER2, HER4, and EGFRvIII. Afatinib used in co-administration with Temozolomide (HY-17364), potently targeting to EGFRvIII-cMet signaling in glioblastoma cells.
    (E/Z)-Afatinib
  • HY-N0392
    Polygalasaponin F
    Inhibitor 99.85%
    Polygalasaponin F is an orally active triterpenoid saponin monomer. Polygalasaponin F downregulates the expression of Bax, p53, caspase-3, NF-κB p65 and MEK1; restores and upregulates the expression of Bcl-2; activates the PI3K/Akt signaling pathway; inhibits the phosphorylation of p38 MAPK, nuclear translocation of NF-κB, TLR4-mediated signaling pathway, mitophagy (Mitophagy) and ROS production; enhances cell viability and suppresses apoptosis (Apoptosis). Polygalasaponin F maintains mitochondrial function, alleviates Ca2+ overload, upregulates pCREB and BDNF, preserves cell viability and inhibits the release of inflammatory cytokines. Polygalasaponin F alleviates lung injury induced by influenza A H1N1 and cerebral ischemia-reperfusion injury. Polygalasaponin F is applicable to researches related to Parkinson's disease, cerebral ischemia, pneumonia induced by influenza A H1N1, stroke and Alzheimer's disease.
    Polygalasaponin F
  • HY-117548
    UNC1062
    Inhibitor 98.92%
    UNC1062 is a highly selective tyrosine kinase (MERTK) inhibitor with an IC50 of 1.1 nM (Morrison Ki = 0.33 nM). UNC1062 exhibits good selectivity for the TAM family (TYRO3 IC50 = 60 nM, AXL IC50 = 85 nM). UNC1062 exhibits significant anti-proliferative effects and induces apoptosis in various cancer models (such as melanoma, gastric cancer, and acute myeloid leukemia). UNC1062 inhibits multiple pathways, including MAPK/ERK, PI3K/AKT and JAK/STAT and affects the motility of head and neck squamous cell carcinoma (HNSCC) cells through the RhoA signaling pathway. UNC1062 inhibits macrophage efferocytosis, and it suitable for research on atherosclerosis.
    UNC1062
  • HY-N2180
    (+)-Eudesmin
    Activator 99.91%
    Pinoresinol dimethyl ether ((+)-Eudesmin) is a non-phenolic furanoid lignin. Pinoresinol dimethyl ether can be isolated from Magnolia biondii. Pinoresinol dimethyl ether activates MAPK, PKC, and PKA upstream pathways and inhibits NO levels. Pinoresinol dimethyl ether has neuroprotective activity.
    (+)-Eudesmin
  • HY-10320A
    Doramapimod hydrochloride
    Inhibitor 98.29%
    Doramapimod hydrochloride (BIRB 796 hydrochloride) is an anti-inflammatory compound with biological activity through inhibition of p38 MAPK. Doramapimod hydrochloride can significantly inhibit the activities of TNF-α and IL-1β induced by LPS, LTA and PGN. Doramapimod hydrochloride showed a stronger inhibitory effect on inflammation induced by all three bacterial toxins, which was more significant compared with the effects of other compounds. Doramapimod hydrochloride can be used in the research of autoimmune diseases.
    Doramapimod hydrochloride
  • HY-112182
    UM-164
    Inhibitor 98.74%
    UM-164 (DAS-DFGO-II) is a highly potent inhibitor of c-Src with a Kd of 2.7 nM. UM-164 also potently inhibits p38α and p38β.
    UM-164
  • HY-169259
    HDAC9-IN-1
    Activator
    HDAC9-IN-1 is a selective class IIa HDAC inhibitor that binds to HDAC9 with an IC50 of 40 nM. HDAC9-IN-1 potently inhibits HDACs 4 and 7 while showing weak activity against HDAC6 (IC50 values: 180 nM (HDAC4), 190 nM (HDAC7), 970 nM (HDAC6)). HDAC9-IN-1 significantly inhibits several human cancer cells, induces apoptosis and DNA damage in human cancer cells, and modulates caspase-related proteins and p38 in human cancer cells. HDAC9-IN-1 can be used for the research of oral cancer, breast cancer, gastric cancer.
    HDAC9-IN-1
  • HY-B2162D
    Chondroitin sulfate (from chicken)
    Inhibitor 99.61%
    Chondroitin sulfate (from chicken) (Chondroitin polysulfate (from chicken)) is an orally active, sulfated linear polysaccharide extracted from chickens, which belongs to glycosaminoglycans. Chondroitin sulfate (from chicken) reduces the phosphorylation levels of ERK1/2 and p38MAPK, inhibits the expression of inflammatory cytokines and MMP, and downregulates the levels of IL-1β, IL-6, TNF-α and PGE2. Chondroitin sulfate (from chicken) improves motor function, protects cartilage tissue, reverses chondrocyte aggregation, and regulates the structure of intestinal flora. Chondroitin sulfate (from chicken) can be used in research related to osteoarthritis.
    Chondroitin sulfate (from chicken)
  • HY-N4202
    Dihydrorotenone
    Activator 99.66%
    Dihydrorotenone is an insecticide and irreversible inhibitor of mitochondrial complex I. Dihydrorotenone may induce Parkinson's disease. Dihydrorotenone induces apoptosis in human plasma cells by triggering endoplasmic reticulum stress and activating the p38 signaling pathway. The oral LD50 of dihydrorotenone in rats is approximately 2.5 g/kg. Dihydrorotenone exhibits insecticide activity and cytotoxicity to plasma cells. Dihydrorotenone can be used to establish animal models of Parkinson's disease, safety assessment of natural pesticides, and potential cancer chemoprevention studies.
    Dihydrorotenone
  • HY-120967
    (2S)-OMPT triethylamine, in ethanol:chloroform (1:1), 98%
    99.0%
    (2S)-OMPT (triethylamine), in ethanol:chloroform (1:1), 98%, Lysophosphatidic acid analogue, is a LPA3 G-protein-coupled receptor agonist. (2S)-OMPT (triethylamine), in ethanol:chloroform (1:1), 98% selectively activates LPA3 G-protein-coupled receptor to trigger downstream cellular signaling events. (2S)-OMPT (triethylamine), in ethanol:chloroform (1:1), 98% induces calcium, IL-6 release in cancer cells and activates MAPK and Akt signaling pathways. (2S)-OMPT (triethylamine), in ethanol:chloroform (1:1), 98% can be used for the research of ovarian cancer.
    (2S)-OMPT triethylamine, in ethanol:chloroform (1:1), 98%
  • HY-N4182
    Licochalcone E
    Inhibitor 99.63%
    Licochalcone E, a flavonoid compound isolated from Glycyrrhiza uralensis, inhibits NF-κB and AP-1 transcriptional activity through the inhibition of AKT and MAPK activation.
    Licochalcone E
  • HY-116626
    SM-7368
    Inhibitor 99.77%
    SM-7368 is a potent NF-kB inhibitor that targets downstream of MAPK p38 activation. SM-7368 inhibits TNF-α-induced MMP-9 upregulation. SM-7368 can be used for the research of chemotherapies targeting TNF-α-mediated tumor invasion and metastasis .
    SM-7368
  • HY-P99866
    Duligotuzumab
    Inhibitor 99.17%
    Duligotuzumab (MEHD-7945A; RG 7597) is a humanized IgG-κ monoclonal antibody targeting EGFR. Duligotuzumab blocks the binding of ligands to these two receptors, inhibits downstream HER/ErbB, AKT and MAPK signaling pathways, induces antibody-dependent cellular cytotoxicity, reduces the proliferation and migration abilities of cancer cells, promotes apoptosis, exerts radiosensitizing effects, and reverses EGFR resistance in cancer cells. Duligotuzumab can be used in tumor-related research.
    Duligotuzumab
  • HY-N2217
    Rotundic acid
    Activator 99.41%
    Rotundic acid is an orally effective triterpenoid with a Kd value of 51.3 µM for PTP1B. Rotundic acid downregulates the AKT/mTOR pro-survival pathway and modulates the MAPK pathway. Rotundic acid induces cell cycle S-phase arrest, DNA damage and apoptosis; it inhibits migration, invasion, angiogenesis and proliferation of cancer cells. Rotundic acid improves leptin sensitivity, regulates gut microbiota and reduces cellular senescence. Rotundic acid can be used in research related to hepatocellular carcinoma, obesity, aging, acute lung injury and type 2 diabetes.
    Rotundic acid
  • HY-N0008
    Orcinol glucoside
    Agonist 99.40%
    Orcinol glucoside is an orally active, blood-brain barrier permeable osteoblast proliferation promoter that targets the Nrf2/Keap1, mTOR and p38 signaling pathways. Orcinol glucoside promotes Nrf2 nuclear translocation, upregulates antioxidant enzyme levels, enhances the phosphorylation of mTOR and p70S6K, and inhibits the enzymatic activity of HAS2 as well as the nuclear translocation of GR. Orcinol glucoside also alleviates oxidative stress, inhibits autophagic flux, osteoclastogenesis and TGF-β1-induced M2 polarization, while reducing collagen deposition and effectively promoting the proliferation, differentiation and mineralization of osteoblasts. Orcinol glucoside also exhibits anti-pulmonary fibrosis, anxiolytic and antidepressant activities. Orcinol glucoside can be used in the research of senile and glucocorticoid-induced osteoporosis, idiopathic pulmonary fibrosis (IPF), anxiety and other related diseases.
    Orcinol glucoside
  • HY-129440
    N-(p-Coumaroyl) Serotonin
    Inhibitor 99.03%
    N-(p-Coumaroyl) Serotonin is an orally active polyphenol found in safflower seeds with potent anti-inflammatory, antioxidant, and antitumor activities. N-(p-Coumaroyl) Serotonin suppresses NF‑κB, TLR4/MyD88 and MAPK signaling, activates NQO1/HO‑1 pathways, and inhibits pro‑inflammatory cytokines, iNOS and COX‑2 and ROS production. N-(p-Coumaroyl) Serotonin induces S‑phase arrest and apoptosis in glioblastoma cells, reduces atherosclerotic lesions, and alleviates renal and vascular injuries. N-(p-Coumaroyl) Serotonin acts as a vasodilator, regulates calcium dynamics. N-(p-Coumaroyl) Serotonin can be used for the research of neurodegenerative diseases, atherosclerosis, glioblastoma, and acute renal failure.
    N-(p-Coumaroyl) Serotonin
  • HY-123961
    SJF-8240
    Degrader 99.33%
    SJF-8240 is a selective p38α PROTAC degrader. SJF-8240 promotes ubiquitination and selective degradation of p38α. SJF-8240 can be used in breast cancer-related research.
    SJF-8240
  • HY-165126
    Schizophyllan
    Inhibitor
    Schizophyllan (SPG) is an orally active extracellular β-glucan produced by the fungus Schizophyllum commune. Schizophyllan improves mitochondrial function and protects against metabolic liver injury by activating the SIRT3 pathway. Schizophyllan inhibits osteoclastogenesis and promotes osteoblast differentiation by suppressing the phosphorylation of JNK/p38, as well as downregulating PGC1β/PPARγ, c-Fos and NFATc1. Recognized via Dectin-1, schizophyllan enables precise delivery of oligonucleotide drugs and antigens to antigen-presenting cells, thus holding great potential in the treatment of inflammatory diseases and vaccine development.
    Schizophyllan
  • HY-N9388
    Andrograpanin
    Inhibitor 99.89%
    Andrograpanin, a bioactive compound from Andrographis paniculata, exhibits anti-inflammatory and anti-infectious properties.
    Andrograpanin
Cat. No. Product Name / Synonyms Species Source
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