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-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-N2423B
    (E/Z)-Sinigrin free base
    Inhibitor
    (E/Z)-Sinigrin ((E/Z)-Allyl-glucosinolate; (E/Z)-2-Propenyl-glucosinolate) free base is an orally active aliphatic thioglucoside anti-leukemia compound. Allyl isothiocyanate, produced by the hydrolysis of (E/Z)-sinigrin free base by myrosinase, has an IC50 of 2.71 μM against HL60 leukemia cells. The hydrolysis products of (E/Z)-sinigrin free base can further activate apoptosis pathways, inhibit NF-κB and MAPK signaling pathways, and induce phase II metabolic enzyme activity, thus exhibiting anti-cancer, anti-inflammatory, antibacterial, antioxidant, and wound healing activities. (E/Z)-Sinigrin free base can be used in research on cancer, inflammation-related diseases (such as atherosclerosis), and infectious diseases. (E/Z)-Sinigrin free base can be naturally extracted from the seeds of Brassica nigra, Brassica juncea, and other Brassicaceae plants such as broccoli and Brussels sprouts. Methyl pechueloate is a guaiane-type sesquiterpene ester compound and a potential precursor of xerantholide. It is useful in the structural elucidation and biosynthetic pathway studies of sesquiterpenoids. Methyl pechueloate can be naturally extracted from the aerial parts of Pechuel-Loeschea leibnitziae (Kuntze) O. Hoffm.
    (E/Z)-Sinigrin free base
  • HY-177155
    p38α-IN-10
    Inhibitor
    P38α-IN-10 (Compound 8) is an orally active inhibitor of p38α, with an IC₅₀ of 230 nM. P38α-IN-10 has an inhibitory effect on TNF production induced by LPS (HY-D1056). P38α-IN-10 can be used for the study of diseases such as rheumatoid arthritis and septic shock.
    p38α-IN-10
  • HY-180324
    Candidone
    Inhibitor
    Candidone is a type of flavanone phenolic compound with anti-cancer and antibacterial activities. Candidone inhibits the proliferation of hepatoblastoma and cholangiocarcinoma cells and induces their apoptosis by up-regulating p21, Bax, and caspase 3/9, and down-regulating Bcl-2 and survivin. It reduces the metastatic ability of cancer cells by inhibiting the expression of phosphorylated p38 and matrix metalloproteinase MMP-9. Candidone has inhibitory effects on multidrug-resistant bacterial strains. Candidone binds to the base pairs of DNA in a groove-binding manner, thereby slightly altering the conformation of DNA.
    Candidone
  • 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-180348
    KFP-H008
    Inhibitor
    KFP-H008 is an orally active potassium-competitive acid blocker. KFP-H008 inhibits gastric acid secretion through blocking H+-K+-ATPase. KFP-H008 reduces ethanol-induced gastric ulcer index and malonaldehyde as well as proinflammatory cytokine expression in vivo. KFP-H008 downregulates p-p38 MAPK and p65 NF-κB expression. KFP-H008 blocks histamine-stimulated acid secretion in rat and dog models. KFP-H008 can be studied in research on acid-related disease, such as ethanol-induced gastric ulcer and gastric epithelial cell damage.
    KFP-H008
  • 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-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-W800535
    Cryptolepine
    Inhibitor
    Cryptolepine is an orally active multi-potent alkaloid with anti-cancer, anti-bacterial, anti-viral, anti-malarial, anti-inflammatory, anti-hyperglycemic, relieve pain and other properties. Cryptolepine acts as an inhibitor of c-Myc, mTOR, NF-κB, HIF-1, MAPK and an activator of AMPKα1/2. It intercalates into DNA, inhibits topoisomerase II (Top II), disrupts mitochondrial dynamics and induces apoptosis. Cryptolepine also exhibits anti-plasmodial and cholinesterase inhibitory activities. Cryptolepine can be used in research related to tumors (melanoma, hepatocellular carcinoma, mammary adenocarcinoma, etc.), malaria, inflammatory diseases and diabetes, particularly in studies focused on inhibiting tumor growth and anti-plasmodial infection.
    Cryptolepine
  • 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-N1988R
    Cucurbitacin IIa (Standard)
    Inhibitor
    Cucurbitacin IIa (Hemslecin A) (Standard) is the analytical standard for Cucurbitacin IIa (HY-N1988). This product is used for research and analytical applications. Cucurbitacin IIa is an orally active, blood-brain barrier-penetrating EGFR inhibitor with an IC50 of 1.455 nM for human EGFR. Cucurbitacin IIa induces caspase-3 dependent cell apoptosis, downregulates survivin expression, enhances autophagy levels, disrupts the actin cytoskeleton through actin aggregation, blocks the cell cycle at the G2/M phase, and inhibits the EGFR-MAPK signaling pathway to exert anti-inflammatory activity. Cucurbitacin IIa can be used in research on inflammatory-related diseases, depression, and non-small cell lung cancer and other cancers.
    Cucurbitacin IIa (Standard)
  • HY-N8712
    Umckalin
    Inhibitor
    Umckalin is Coumarin (HY-N0709) derivative that exhibits anti-inflammatory properties. Umckalin reduces phosphorylation of p38 MAPK, JNK, and ERK, lowers TNF-α, IL-6, IL-1β, NO, and PGE2 production. Umckalin can be used for the research of chronic inflammatory diseases.
    Umckalin
  • 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)
  • HY-172406
    MAPK-IN-4
    Inhibitor
    MAPK-IN-4 (Compound c1) is an orally active anti-inflammatory agent. MAPK-IN-4 can inhibit the expression and release of pro-inflammatory cytokines IL-6 and TNF-α induced by LPS (HY-D1056). MAPK-IN-4 can bind to IRAK4 and exert its anti-inflammatory effect by inhibiting the MAPK pathway.
    MAPK-IN-4
  • HY-158334
    NDs-IN-1
    Inhibitor
    (Neurodegenerative diseases) NDs-IN-1 (Compound 3g) inhibits the activities of key enzymes such as hBACE-1, hAChE and hMAO-B. NDs-IN-1 is a novel non-covalent multi-target inhibitor. NDs-IN-1 is mainly used in the study of neurodegenerative diseases.
    NDs-IN-1
Cat. No. Product Name / Synonyms Species Source
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