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-175666
    ISAM-CG557
    Activator
    ISAM-CG557 is a selective CB2R agonist, with a Ki of 54.6 nM. ISAM-CG557 reduces intracellular ROS levels and caspase activity. ISAM-CG557 exhibits significant MAPK bias and moderate G-protein bias, with CB2R EC50s of 0.60 nM (cAMP), 60.9 nM (β-arrestin) and 0.03 nM (MAPK). ISAM-CG557 exerts potent anti-inflammatory effects by reducing pro-inflammatory cytokines and increasing anti-inflammatory cytokines in cells. ISAM-CG557 can be used for the study of neuroinflammatory and neurodegenerative disorders.
    ISAM-CG557
  • HY-N3584R
    Paris saponin VII (Standard)
    Inhibitor
    Paris saponin VII (Standard) is the analytical standard of Paris saponin VII. This product is intended for research and analytical applications. Paris saponin VII (Chonglou Saponin VII) is a steroidal saponin isolated from the roots and rhizomes of Trillium tschonoskii. Paris saponin VII-induced apoptosis in K562/ADR cells is associated with Akt/MAPK and the inhibition of P-gp. Paris saponin VII attenuates mitochondrial membrane potential, increases the expression of apoptosis-related proteins, such as Bax and cytochrome c, and decreases the protein expression levels of Bcl-2, caspase-9, caspase-3, PARP-1, and p-Akt. Paris saponin VII induces a robust autophagy in K562/ADR cells and provides a biochemical basis in the treatment of leukemia.
    Paris saponin VII (Standard)
  • HY-10406B
    rel-Talmapimod hydrochloride
    Inhibitor
    rel-Talmapimod (rel-SCIO-469) hydrochloride is an orally active and selective inhibitor of p38α MAPK with an IC50 of 9 nM. rel-Talmapimod hydrochloride inhibits the secretion of inflammatory factors (such as TNFα, IL-1β, IL-6, and VEGF) by suppressing the p38α MAPK pathway, and it also inhibits angiogenesis and osteoclast activation. rel-Talmapimod hydrochloride inhibits the growth of multiple myeloma cells and induces apoptosis. rel-Talmapimod hydrochloride can be used to study various hematological malignancies (such as multiple myeloma, myelodysplastic syndrome).
    rel-Talmapimod hydrochloride
  • HY-163114
    2-Stearoxyphenethyl phosphocholin
    Inhibitor
    2-Stearoxyphenethyl phosphocholin (compound 1a) is a p38 MAPK inhibitor with anticancer activity. 2-Stearoxyphenethyl phosphocholin may bind to the p38 MAPK lipid-binding pocket and has broad-spectrum anti-tumor and lipid-modulating activities.
    2-Stearoxyphenethyl phosphocholin
  • HY-169067
    10-Methoxy-canthin-6-one
    Activator 98.71%
    10-Methoxy-canthin-6-one (Mtx-C) is analkaloid derivative. 10-Methoxy-canthin-6-one can induce DNA damage by intercalating into DNA. 10-Methoxy-canthin-6-one can inhibit cancer cells proliferation, cause G2/M phase arrest and induce myeloid differentiation. T10-Methoxy-canthin-6-one can upregulate the expression of myeloperoxidase, CD15, CD11b, and CD14, as well as activation of p38 MAPK. 10-Methoxy-canthin-6-one also exhibits anti-bacterial activity. 10-Methoxy-canthin-6-one can be used for the researches of cancer and infection, such as acute myeloid leukemias (AML).
    10-Methoxy-canthin-6-one
  • HY-175037
    DNH28
    Inhibitor
    DNH28 is a potent NF-κB and MAPK inhibitor with an IC50 of 0.93 μM against HepG2 cells. DNH28 promotes apoptosis by down-regulating the expression of Bcl-2, up-regulating the expression of BAX and Cleaved-caspase-3. DNH28 blocks the cell cycle and inhibits migration. DNH28 can be used for the study of hepatocellular carcinoma (HCC).
    DNH28
  • HY-108346
    JX401
    Inhibitor
    JX401 is a potent inhibitor of p38alpha, containing a 4-benzylpiperidine motif. p38alpha is hyperactive in inflammatory diseases, and various indications suggest that its inhibition would reverse inflammation. JX401 has the potential for the research of inflammation.
    JX401
  • HY-147518
    p38-α MAPK-IN-5
    Inhibitor
    p38-α MAPK-IN-5 (compound 4e) is a potent p38α inhibitor with IC50s of 0.1 nM, 0.2 nM, 944 nM, 4100 nM for p38α, p38 β, p38γ, p38δ, respectively. p38-α MAPK-IN-5 has anti-inflammatory effect. p38-α MAPK-IN-5 has the potential for asthma and chronic obstructive pulmonary disease (COPD) research.
    p38-α MAPK-IN-5
  • HY-106159
    SB-T-101141
    SB-T-101141 is a novel taxane. SB-T-101141 effectively induces a noncanonical ferroptosis to overcome Paclitaxel (HY-B0015) resistance of breast cancer. SB-T-101141 facilitates the production of iron and ferrous ions and ROS. SB-T-101141 stably binds to KHSRP to inhibit the iron-dependent expression of CISD1 related to iron homeostasis. SB-T-101141 synergistically enhances the iron-dependent activation of JNK and PERK pathways via KHSRP. SB-T-101141 suppresses breast tumor growth in MCF-7(PR)/MDA-MB-231(PR) or KHSRP knock-down MCF-7 xenograft mice model.
    SB-T-101141
  • HY-A0129R
    Histamine phosphate (Standard)
    Activator
    Histamine phosphate (Standard) is the analytical standard of Histamine phosphate (HY-A0129). This product is intended for research and analytical applications. Histamine phosphate is the agonist for histamine receptor and a vasodilator. Histamine phosphate is an organic nitrogen compound that participates in local immune responses, regulates intestinal physiological functions, and acts as a neurotransmitter. Histamine phosphate affects p38 MAPK/Akt signaling pathway, exhibits antitumor, antioxidant and anti-inflammatory activities. Histamine phosphate can be used in the research of acute myeloid leukemia, malignant melanoma, and renal cell carcinoma.
    Histamine phosphate (Standard)
  • HY-18861
    BIRB-1017
    Inhibitor
    BIRB-1017 is a potent inhibitor of p38 MAP kinase. BIRB-1017 can be used in inflammation research.
    BIRB-1017
  • HY-18794
    R-03201195
    Inhibitor
    R-03201195 is an efficient and selective p38 MAP kinase inhibitor with an IC50 for p38α of 0.7 nM. R-03201195 has inhibitory activity against TNF-α in THP-1 cells and against IL-1β in human whole blood, with IC50 values of 0.25 and 0.57 nM respectively. R-03201195 can be used for inflammatory diseases such as rheumatoid arthritis.
    R-03201195
  • HY-121033
    BS148
    Activator
    BS148 is a selective sigma-2 receptor (S2R) agonist with a Ki 20 nM. BS148 shows >80-fold selective for S2R than S1R. BS148 activates the endoplasmic reticulum stress response through the upregulation of protein kinase R-like ER kinase (PERK), activating transcription factor 4 (ATF4) genes, and C/EBP homologous protein (CHOP). BS148 induces apoptosis in melanoma cell. BS148 downregulates genes related to the cholesterol pathway and activates the MAPK signaling pathway. BS148 can be used for the study of melanoma.
    BS148
  • HY-177156
    Glucagon receptor antagonist-8
    Antagonist
    Glucagon receptor antagonist-8 (Compound 1) is a human glucagon receptor and p38 mitogen-activated protein (MAP) kinase antagonist, with IC50s of 0.27 μM and 0.16 μM, respectively.
    Glucagon receptor antagonist-8
  • HY-45124
    3-Fluoro-desmethyl-cabozantinib
    Ligand
    3-Fluoro-desmethyl-cabozantinib is an BCL6 ligand that can be used in the synthesis of PROTACs, such as SJF-8240 (HY-123961). 3-Fluoro-desmethyl-cabozantinib is also a p38α ligand that can be used to synthesize PROTACs, such as SJFα (HY-114404).
    3-Fluoro-desmethyl-cabozantinib
  • HY-180922
    EGFR kinase-IN-8
    Inhibitor
    EGFR kinase-IN-8 (Compound H8b) is an EGFR inhibitor. EGFR kinase-IN-8 potently inhibits both triple-mutated EGFRL858R/T790M/C797S (IC50 = 3.86 nM) and double-mutated EGFRL858R/T790M (IC50 = 1.23 nM). EGFR kinase-IN-8 suppresses EGFR phosphorylation and downstream AKT, STAT3, and MAPK signaling. EGFR kinase-IN-8 exhibits anticancer activity against non-small cell lung cancer.
    EGFR kinase-IN-8
  • HY-175782
    SMU-R39
    Inhibitor
    SMU-R39 is a TLR7 and TLR8 antagonist with IC50 values of 3.22 μM and 0.24 μM, respectively. SMU-R39 binds to recombinant mTLR7 protein (KD = 2.36 μM) and to recombinant hTLR8 protein (KD = 105 nM). SMU-R39 suppresses downstream NF-κB and MAPK signaling, and reduces secretion/transcription of pro-inflammatory cytokines (TNF-α, IL-1β, IL-6) in PBMCs and THP-1 cells. SMU-R39 demonstrates anti-inflammatory efficacy in Imiquimod (IMQ) (HY-B0180)-induced psoriasis mouse model. SMU-R39 can be used for the study of autoimmune diseases such as psoriasis.
    SMU-R39
  • HY-N19847
    LYRM03
    Inhibitor
    LYRM03 is a derivative of Ubenimex (HY-B0134) and a Aminopeptidase N inhibitor. LYRM03 is isolated from Streptomyces HCCB10043. LYRM03 inhibits TLR4, MyD88, NLRP3, ASC, NF-κB and p38 MAPK, stabilizes IκB, and suppresses LPS-induced expression of iNOS and COX-2. LYRM03 reduces the levels of inflammatory cytokines and oxidative stress markers, and alleviates pulmonary edema. LYRM03 exhibits anticancer activity against breast cancer. LYRM03 has anti-inflammatory activity. LYRM03 can be used in the research of acute lung injury and breast cancer.
    LYRM03
  • HY-B0736AR
    Sertaconazole nitrate (Standard)
    Activator
    Sertaconazole (nitrate) (Standard) is the analytical standard of Sertaconazole (nitrate). This product is intended for research and analytical applications. Sertaconazole nitrate (FI7056) is a broad-spectrum topical antifungal agent, exhibits anti-inflammatory activity via activation of a p38-COX-2-PGE2 pathway. Sertaconazole nitrate is also a microtubule inhibitor, shows antiproliferative effect, induces apoptosis and autophagy, and can also inhibit the migration of cells.
    Sertaconazole nitrate (Standard)
  • HY-175433
    p38 MAPK-IN-10
    Inhibitor
    p38 MAPK-IN-10 (Compound 4) is an orally active and potent p38 MAP kinase inhibitor (IC50=570 nM). p38 MAPK-IN-10 is promising for research of chronic inflammatory diseases such as rheumatoid arthritis and Crohn’s disease.
    p38 MAPK-IN-10
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