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-149921
    Antiangiogenic agent 3
    Inhibitor
    Antiangiogenic agent 3 (compound 3) is a potent antiangiogenic agent. Antiangiogenic agent 3 is an inhibitor of human umbilical vein endothelial cells (HUVEC). Antiangiogenic agent 3 inhibits HUVEC migration and chemotactic motilities. Antiangiogenic agent 3 also decreases the gene expression of Src, cdc42, and MAPK.
    Antiangiogenic agent 3
  • HY-120485
    Raxofelast
    Inhibitor
    Raxofelast (IRFI-016) is an antioxidant agent in various models of ischemia-reperfusion injury. Raxofelast has antiproliferative activity in H2O2-stimulated rat aortic smooth muscle cells. Raxofelast attenuates the activation of mitogen-activating protein kinase (MAPK), ERK kinase 1, 2 (MEK1,2) and protein kinase C (PKC) without affecting Ras expression.
    Raxofelast
  • HY-N0735R
    Phellodendrine chloride (Standard)
    Inhibitor
    Phellodendrine chloride (Standard) is the analytical standard of Phellodendrine chloride (HY-N0735). Phellodendrine chloride is an orally active plant alkaloid. Phellodendrine chloride inhibits the proliferation of KRAS-mutated pancreatic cancer cells by suppressing macropinocytosis and glutamine metabolism, inducing ROS accumulation and mitochondrial apoptosis. Phellodendrine chloride promotes autophagy by activating the AMPK/mTOR pathway, alleviating intestinal damage in ulcerative colitis. Phellodendrine chloride can alleviate gouty arthritis by inhibiting the IL-6/STAT3 signaling pathway. Phellodendrine chloride suppresses allergic reactions by altering the conformation of MRGPRB3/MRGPRX2 protein, thereby inhibiting the activation of PKC and subsequent downstream MAPK and NF-κB signaling. Phellodendrine chloride inhibits the AKT/NF-κB pathway and down-regulates the expression of COX-2, thereby protecting zebrafish embryos from oxidative stress. Phellodendrine chloride has an anti-major depressive disorder (MDD) effect by down-regulating CHRM1, HTR1A, and the PI3K/Akt signaling pathway.
    Phellodendrine chloride (Standard)
  • HY-172409
    CB1R antagonist 2
    Inhibitor
    CB1R antagonist 2 (Compound 11g) is the antagonist for cannabinoid receptor 1 (CB1R), that inhibits MAPK/NF-κB signaling pathway and exhibits anti-inflammatory activity. CB1R antagonist 2 inhibits LPS (HY-D1056)-induced IL-6, IL-1β and TNF-α expressions in RAW264.7. CB1R antagonist 2 ameliorates OVA-induced allergic rhinitis in mouse models.
    CB1R antagonist 2
  • HY-172209
    PPIA-IN-1
    Inhibitor
    PPIA-IN-1 (Compound 20b) is the inhibitor for peptidylprolyl isomerase A (PPIA) with a KD of 0.52 μM. PPIA-IN-1 exhibits antiproliferative activity in a variety of cancer cell lines (IC50 for HCT116 is 0.69 μM), arrests the cell cycle at G0/G1 phase, and exhibits anti-metastatic effect in cell HCT116. PPIA-IN-1 increases ROS, causes DNA damage, ER stress and mitochondrial dysfunction, inducing apoptosis in HCT116 through MAPK pathway. PPIA-IN-1 exhibits antitumor activity in mouse CT26 xenograft models.
    PPIA-IN-1
  • HY-W018197R
    2-Phenylacetamide (Standard)
    Inhibitor
    2-Phenylacetamide (Standard) is the analytical standard of 2-Phenylacetamide. This product is intended for research and analytical applications. 2-Phenylacetamide is a estrogen-like compound that can be isolated from Lepidium apetalum seeds. 2-Phenylacetamide inhibits p38 MAPK signaling pathway, exhibits anti-inflammatory, antioxidant, anti-hypertensive, and anti-fibrosis effects. 2-Phenylacetamide is orally active.
    2-Phenylacetamide (Standard)
  • HY-108642A
    AMG-548 hydrochloride
    Inhibitor
    AMG-548 hydrochloride, an orally active and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γ and p38δ. AMG-548 hydrochloride is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM). AMG-548 hydrochloride inhibits Wnt signaling by directly inhibiting Casein kinase 1 isoforms δ and ε.
    AMG-548 hydrochloride
  • HY-N0755R
    Rhoifolin (Standard)
    Activator
    Rhoifolin (Standard) is the analytical standard of Rhoifolin. This product is intended for research and analytical applications. Rhoifolin is a flavone glycoside can be isolated from Rhus succedanea. Rhoifolin has anti-diabetic effect acting through enhanced adiponectin secretion, tyrosine phosphorylation of insulin receptor-β and glucose transporter 4 (GLUT 4) translocation. Rhoifolin has an anti-inflammatory action via multi-level regulation of inflammatory mediators. Rhoifolin ameliorates titanium particle-stimulated osteolysis and attenuates osteoclastogenesis via RANKL-induced NF-κB and MAPK pathways. Rhoifolin also has cytotoxic activity against different cancer cell lines.
    Rhoifolin (Standard)
  • HY-178059
    FGFR-IN-23
    Inhibitor
    FGFR-IN-23 (Compound 9p) is a covalent pan FGFR inhibitor with IC50s of 14, 4.2, 5 and 220 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively. FGFR-IN-23 also has potent inhibitory activity against gatekeeper mutants, such as FGFR1V561M and FGFR3V555M. FGFR-IN-23 suppresses the activation of FGFR-mediated signaling and induces apoptosis. FGFR-IN-23 shows significant antitumor efficacy in RT112 xenograft mouse models. FGFR-IN-23 can be used for cancers and its drug resistance research.
    FGFR-IN-23
  • HY-177320
    p38 Kinase-IN-9
    Inhibitor
    p38 Kinase-IN-9 (example 4) is a p38 kinase inhibitor with an IC50 of <1 μM. p38 Kinase-IN-9 can be used for the study of p38 kinase mediated diseases, including inflammatory diseases.
    p38 Kinase-IN-9
  • HY-172807
    p38α-IN-9
    Inhibitor
    p38α-IN-9 (Compound 2015) is a p38α inhibitor and blocks p38α’s enzymatic activity with an IC50 lower than 20 nM. p38α-IN-9 inhibits MK2T334 phosphorylation. p38α-IN-9 activates Cdc25b and Cdc25c and simultaneously inactivates Wee1, leading to mitotic catastrophe, aneuploidy or polyploidy and DNA damage. p38α-IN-9 Inhibits colorectal cancer (CRC) metastasis.
    p38α-IN-9
  • HY-N15742
    Talaroconvolutin A
    Inhibitor
    Talaroconvolutin A is a ferroptosis inducer. Talaroconvolutin A induces ferroptosis by increasing reactive oxygen species (ROS) levels rather than the GPX4 pathway. Talaroconvolutin A downregulates the expression of the channel protein solute carrier family 7 member 11 (SLC7A11) and upregulates arachidonic acid lipoxygenase 3 (ALOXE3). Talaroconvolutin A inhibits the growth of colorectal cancer cells HCT116 and bladder cancer cells SW480 with IC50 values of 1.22 μM and 1.4 μM, respectively. Talaroconvolutin A can be used in the study of colorectal cancer and bladder cancer[1][2][3].
    Talaroconvolutin A
  • HY-N0311R
    Emodin-8-glucoside (Standard)
    Inhibitor
    Emodin-8-glucoside (Standard) is the analytical standard of Emodin-8-glucoside. This product is intended for research and analytical applications. Emodin-8-glucoside is an anthraquinone derivative that can be isolated from Aloe vera. Emodin-8-glucoside is the inhibitor for MAPK with an inhibition constant of 430.14 pM. Emodin-8-glucoside exhibits moderate inhibitory activity against rat lens aldose reductase (ALAR) and topoisomerases II with IC50s of 14.4 μM and 66 μM. Emodin-8-glucoside exhibits antioxidant, anti-inflammatory and anti-fibrotic activities. Emodin-8-glucoside can cross the blood brain barrier.
    Emodin-8-glucoside (Standard)
  • HY-125807
    IS20
    Activator
    IS20 is a Prokineticin receptor 1 (PKR1) agonist. IS20 diminishes Doxorubicin (HY-15142A) mediated apoptosis and ROS production by activating Akt or MAPK pathways. IS20 protects the heart against Doxorubicin-induced cardiovascular toxicity and improves the survival rate and cardiac function in mouse models. IS20 does not alter the cytotoxicity and antitumor activity of acute DOX treatment in breast cancer cells and MDA-MB-231 xenograft mouse models. IS20 can be used for cancers research.
    IS20
  • HY-136778
    INH2BP
    Activator
    INH2BP is a poly(ADP-ribose) polymerase (PARP) inhibitor with antioxidant and anti-apoptotic activities. INH2BP reduces the production of intracellular reactive oxygen species (ROS), modulates the expression of apoptosis-related proteins such as Bax, Bcl-2 and cleaved caspase-3 and enhances cell survival through the activation of the ERK1/2 and p38 MAPK signaling pathways. INH2BP is promising for research of cardiovascular diseases.
    INH2BP
  • HY-101268
    CHMFL-ABL-053
    Inhibitor
    CHMFL-ABL-053 (Compound 18a) is a potent, selective, and orally available BCR-ABL, SRC and p38 kinase inhibitor with IC50 values of 70, 90 and 62 nM against ABL1, SRC and p38, respectively.
    CHMFL-ABL-053
  • HY-15509
    Semapimod
    Semapimod, an inhibitor of proinflammatory cytokine production, can inhibit TNF-α, IL-1β, and IL-6. Semapimod inhibits TLR4 signaling (IC50≈0.3 μM). Semapimod inhibits p38 MAPK and nitric oxide production in macrophages. Semapimod has potential in a variety of inflammatory and autoimmune disorders.
    Semapimod
  • HY-111214
    K-14585
    Inhibitor
    K-14585 is a peptide competitive PAR2 antagonist. K-14585 inhibits PAR2-dependent IL-8 production, NF-κB phosphorylation, and p38 signaling. K-14585 reduces SLIGKV (PAR2 agonist peptide)-induced Ca2+ mobilisation in primary human keratinocytes.
    K-14585
  • HY-N7255R
    Cycloartenol (Standard)
    Inhibitor
    Cycloartenol (Standard) is the analytical standard of Cycloartenol. This product is intended for research and analytical applications. Cycloartenol, a phytosterol compound, is one of the key precusor substances for biosynthesis of numerous sterol compounds. Cycloartenol inhibits the migration of glioma cells and suppresses the phosphorylation of the p38 MAP kinase. Cycloartenol has a variety of pharmacological activities such as anti-inflammatory, anti-tumor, antioxidant, antibiosis and anti-alzheimer's disease. Cycloartenol also plays an important role in the process of plant growth and development.
    Cycloartenol (Standard)
  • HY-76006R
    3-Hydroxybenzaldehyde (Standard)
    Inhibitor
    3-Hydroxybenzaldehyde (Standard) is the analytical standard of 3-Hydroxybenzaldehyde. This product is intended for research and analytical applications. 3-Hydroxybenzaldehyde (3-HBA) is a precursor compound for phenolic compounds like Protocatechuic aldehyde (PCA) (HY-N0295). 3-Hydroxybenzaldehyde, produced by 3-hydroxybenzyl-alcohol dehydrogenase, is a substrate of aldehyde dehydrogenase (ALDH) in rats and humans. 3-Hydroxybenzaldehyde has vasculoprotective effects in vitro and in vivo. 3-Hydroxybenzaldehyde is proming for research of atherosclerosis[1][2][3][4].
    3-Hydroxybenzaldehyde (Standard)
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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