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-175431
    p38 MAPK-IN-8
    Inhibitor
    p38 MAPK-IN-8 (Compound 8) is an orally active, potent and selective p38 mitogen-activated protein kinase (p38 MAPK) inhibitor. p38 MAPK-IN-8 is promising for research of inflammatory responses, autoimmune diseases, and cancer.
    p38 MAPK-IN-8
  • HY-176019
    Methylcarbamyl PAF C-8
    Activator
    Methylcarbamyl PAF C-8 is resistant to the degradation function of platelet-activating factor acetylhydrolase (PAF-AH). It has a half-life of more than 100 minutes in platelet-poor plasma and possesses the activity of inducing platelet aggregation. In NRK-49 cells overexpressing the PAF receptor, Methylcarbamyl PAF C-8 can induce the expression of c-myc and c-fos, and activate mitogen-activated protein kinase (MAPK). Additionally, Methylcarbamyl PAF C-8 can induce cell cycle arrest in the G1 phase. Methylcarbamyl PAF C-8 holds promise for research in the fields of cardiovascular diseases and anti-cancer therapy.
    Methylcarbamyl PAF C-8
  • HY-E70759
    MKK6 SDTD Recombinant Human Active Protein Kinase
    The mitogen-activated protein kinase kinase 6 (MKK6) is one of the upstream activators of p38 MAPK. MKK6 activates myocardial cell NF-κB and inhibits apoptosis in a p38 MAPK-dependent manner. MKK6 SDTD is a mutant of MKK6. MKK6 SDTD Recombinant Human Active Protein Kinase is a recombinant MKK6 SDTD protein that can be used to study MKK6 SDTD-related functions.
    MKK6 SDTD Recombinant Human Active Protein Kinase
  • HY-P10414
    Klotho-derived peptide 1
    Inhibitor
    Klotho-derived peptide 1 (KP1 human) blocks TGF-β/TGF-β receptor 2 interaction, inhibits TGF-β-induced activation of Smad2/3 and mitogen-activated protein kinase (MAPK), and exhibits anti-fibrotic and kidney protective effects in mouse model.
    Klotho-derived peptide 1
  • HY-174858
    dASK1-VHL
    Inhibitor
    dASK1-VHL is an orally active PROTAC degrader targeting ASK1. dASK1-VHL can effectively bind VHL and promote the selective degradation of ASK1. dASK1-VHL effectively reduces ASK1 protein levels, inhibits the activation of p38 MAPK, and reduces liver lipid content. dASK1-VHL provides new ideas for the study of Metabolic dysfunction-associated steatohepatitis (MASH) (Pink: ASK1 ligand 1 (HY-174860); Blue: E3 ligand (S,R,S)-AHPC (HY-125845); Black: Linker, (S,R,S)-AHPC-CO-C2-PEG-NHCO-C2-COOH (HY-174861).
    dASK1-VHL
  • HY-175764
    FIP22
    Inhibitor
    FIP22 is a potent and selective IRAK4 PROTAC degrader (HEK293T cells: DC50 = 3.2 nM; THP-1 cells: DC50 = 10.6 nM). FIP22 induces the ubiquitin-proteasome system by forming an IRAK4-FIP22-CRBN ternary complex (EC50 = 12.63 nM), thereby potently blocking IRAK4-mediated NF-κB and MAPK signaling pathways. FIP22 can be used for the study of atopic dermatitis (Pink: IRAK4 ligand (HY-175765); Blue: CRBN ligand (HY-W087383); Black: Linker (HY-46871)).
    FIP22
  • HY-N16118
    Asperosaponin V
    Modulator
    Asperosaponin V is an indirect modulator of bone metabolism-related targets (e.g., PI3K/AKT, BMP-2/p38, and ERK 1/2 pathways). Asperosaponin V promotes marrow stromal cell proliferation and induces osteoblast differentiation. Asperosaponin V is promising for research of osteoporosis and fracture healing.
    Asperosaponin V
  • HY-174377
    PeS-9
    Inhibitor

    PeS-9 is an Androgen Receptor (AR) degrader that induces androgen receptor degradation PeS-9 induces mitochondrial and ER stress by promoting cytotoxic ROS production, leading to the release of mitochondrial cytochrome C and AIF. PeS-9 subsequently activates caspases-9 and -3, causing DNA fragmentation and apoptotic cell death. PeS-9 has anticancer activity against prostate cancer and exerts in vivo antitumor and antimetastatic activity with minor side effects. PeS-9 can be used for the study of targeting monotherapy against GLUT-1-overexpressing tumors.

    PeS-9
  • HY-172803
    Ferroptosis inducer-7
    Activator
    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.
    Ferroptosis inducer-7
  • HY-P3918
    EGF-R (661-681) T669 Peptide
    EGF-R (661-681) T669 Peptide is a MAPK substrate that can used to measure MAPK catalytic activity.
    EGF-R (661-681) T669 Peptide
  • HY-176786
    MCB-36
    Inhibitor
    MCB-36 is a VHL-recruiting pan-KRAS PROTAC degrader without affecting KRAS transcription. MCB-36 exhibits minimal effects on HRAS and NRAS protein levels. MCB-36 binds to the GDP-loaded state of G12D, G12C, G12V, and wild-type KRAS with high affinities Kd ≈ 1 pM). MCB-36 decreases p-ERK levels, leading to cell apoptosis. MCB-36 effectively suppress KRASG12C inhibitor-resistant cancer cells and remodel the tumor immune microenvironment. MCB-36 can be used for the study of colorectal cancer and lung cancer (Pink: Target protein ligand; Blue: E3 ligand (HY-112078); Black: Linker (HY-W091879)).
    MCB-36
  • HY-17003R
    Saquinavir mesylate (Standard)
    Inhibitor
    Saquinavir mesylate (Standard) (Ro 31-8959/003 (Standard)) is the analytical standard of Saquinavir mesylate (HY-17003). This product is intended for research and analytical applications. Saquinavir (Ro 31-8959) mesylate is an orally active HIV protease inhibitor that can be used in the research of AIDS. Saquinavir mesylate also has anti-inflammatory activity and can induce apoptosis of human red blood cells.
    Saquinavir mesylate (Standard)
  • HY-10320G
    Doramapimod (GMP)
    Inhibitor
    Doramapimod GMP (BIRB 796 GMP) is an orally active inhibitor for p38 MAPK, with IC50s of 38, 65, 200 and 520 nM, for p38α, p38β, p38γ, p38δ. Doramapimod exhibits cytotoxicity and antitumor activity against multiple myeloma, synergizes with multidrug resistance protein 1 (ABCB1) and aurora kinase inhibitor VX680, promoting their antitumor efficacy against oral epidermoid carcinoma and cervical cancer. Doramapimod also exhibits anti-inflammatory activity.
    Doramapimod (GMP)
  • HY-174437B
    FLT3-IN-32 hydrochloride
    Inhibitor
    FLT3-IN-32 hydrochloride is a potent and orally active FLT3 inhibitor with an IC50s of 0.29 nM, 0.77 nM and 2.07 nM against FLT3-ITD, FLT3-D835Y and FLT-N676K. FLT3-IN-32 hydrochloride reduces the phosphorylation of FLT3 and its downstream signaling molecules (STAT5, MAPK, AKT) to induce FLT3-mutated Ba/F3 cells apoptosis. FLT3-IN-32 hydrochloride shows significant anti-tumor efficacy in n the MV4-11 xenograft model. FLT3-IN-32 hydrochloride can be used for the study of acute myeloid leukemia (AML).
    FLT3-IN-32 hydrochloride
  • HY-N0168AR
    (Rac)-Hesperetin (Standard)
    Activator
    (Rac)-Hesperetin (Standard) is the analytical standard of (Rac)-Hesperetin. This product is intended for research and analytical applications. (Rac)-Hesperetin is the racemate of Hesperetin. Hesperetin is a natural flavanone that can be found in citrus, and acts as a potent and orally active broad-spectrum inhibitor against human UGT activity. Hesperetin induces apoptosis via p38 MAPK activation. Hesperetin displays a range of bioactivities including antioxidant, anti-inflammatory, and anti-cancer. Hesperetin is found to induce cell-cycle arrest at G2/M phase. Hesperetin can reduce Bcl-2 and enhance BaxM. Hesperetin induces apoptosis through inhibiting NF-κB receptor.
    (Rac)-Hesperetin (Standard)
  • HY-10261AR
    Afatinib dimaleate (Standard)
    Inhibitor
    Afatinib (dimaleate) (Standard) is the analytical standard of Afatinib (dimaleate). This product is intended for research and analytical applications. Afatinib (BIBW 2992) dimaleate is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively. Afatinib dimaleate can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer.
    Afatinib dimaleate (Standard)
  • HY-N1506R
    Ganodermanontriol (Standard)
    Modulator
    Karbutilate (Standard) is the analytical standard of Karbutilate. This product is intended for research and analytical applications. Karbutilate (NIA-11092) is a nonselective soil-active herbicide which is used to kill one-leaf pinyon saplings.
    Ganodermanontriol (Standard)
  • HY-114422
    ARRY-371797
    Inhibitor
    ARRY-371797 is a potent and orally active p38α MAPK and BChE inhibitor with IC50 values of 12.0, 0.13, >100 µM for p38α MAP, hBChE, hAChE, respectively. ARRY-371797 has the potential for the research of Alzheimer’s disease.
    ARRY-371797
  • HY-168482
    NF-κB/MAPK-IN-2
    Inhibitor
    NF-κB/MAPK-IN-2 (compound 14) is a potent NF-κB and MAPK Inhibitor. NF-κB/MAPK-IN-2 decreases the protein expression of p-p65, p-IκB, p-p38, p-JNK, and p-ERK. NF-κB/MAPK-IN-2 reduces the LPS-induced release of TNF-α and IL-6. NF-κB/MAPK-IN-2 inhibits nuclear translocation of p65 and c-Fos. NF-κB/MAPK-IN-2 has the potential for the research of sepsis.
    NF-κB/MAPK-IN-2
  • HY-B0558R
    Carbimazole (Standard)
    Inducer
    Carbimazole (Standard) is the analytical standard of Carbimazole. This product is intended for research and analytical applications. Carbimazole is an orally active antithyroid agent which rapidly converts to Methimazole after absorption and prevents thyroid peroxidase enzyme from iodinating and coupling the tyrosine residues on thyroglobulin, hence reducing the production of thyroxine. Carbimazole also displays anti-inflammatory and neuronal-protective activities, suggesting its application for hyperthyroidism and neurological research.
    Carbimazole (Standard)
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