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

p38 MAPK

p38 MAPK

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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.

p38 MAPK Isoform Specific Products:

p38 MAPK Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • 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-172807
    p38α inhibitor 9
    		Inhibitor
    p38α inhibitor 9 (Compound 2015) is a p38α inhibitor and blocks p38α’s enzymatic activity with an IC50 lower than 20 nM. p38α inhibitor 9 inhibits MK2T334 phosphorylation. p38α inhibitor 9 activates Cdc25b and Cdc25c and simultaneously inactivates Wee1, leading to mitotic catastrophe, aneuploidy or polyploidy and DNA damage. p38α inhibitor 9 Inhibits colorectal cancer (CRC) metastasis.
    p38α inhibitor 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-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-10261R
    Afatinib (Standard)
    		Inhibitor
    Afatinib (Standard) is the analytical standard of Afatinib. This product is intended for research and analytical applications. Afatinib (BIBW 2992) 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 can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer.
    Afatinib (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-N9955
    Isonardosinone
    		Inhibitor
    Isonardosinone is a nardosinone-type sesquiterpenes, which can be isolated from Valerianaceae. Isonardosinone inhibits NF-κB and MAPK signaling pathway, suppresses expression of iNOS and cyclooxygenase-2 (COX-2) in Lipopolysaccharides (HY-D1056)-induced BV2 microglia, exhibits anti-inflammatory activity.
    Isonardosinone
  • HY-N13294
    Cernuumolide J
    		Activator
    Cernuumolide J (TMJ-105) is an JAK2/STAT3 inhibitor. Cernuumolide J induces G2/M phase arrest and apoptosis in HEL leukemia cells by downregulating the phosphorylation of JAK2, STAT3, and Erk, and activating the phosphorylation of JNK and p38 MAPK. Cernuumolide J inhibits HEL leukemia cell growth in a time- and concentration-dependent manner, with an IC50 value of 1.79 μM. Cernuumolide J can be used for research in the field of anti-cancer therapy.
    Cernuumolide J
  • HY-N0202R
    Atractylenolide II (Standard)
    		Activator
    Atractylenolide II (Standard) is the analytical standard of Atractylenolide II. This product is intended for research and analytical applications. Atractylenolide II (Asterolide) is a sesquiterpenoid compound. Atractylenolide II can induce G1 phase cell cycle arrest and apoptosis in B16 melanoma cells. Atractylenolide II is an orally effective anticancer agent that can exert anti-melanoma effects by inhibiting the STAT3 signaling pathway. In addition, Atractylenolide II has been shown to ameliorate myocardial fibrosis, oxidative stress, and neuroprotective activity.
    Atractylenolide II (Standard)
  • 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
  • HY-17007S
    Saquinavir-d9
    		Inhibitor
    Saquinavir-d9 (Ro 31-8959-d9) is the deuterium labeled Saquinavir (HY-17007). Saquinavir (Ro 31-8959) is an orally active HIV protease inhibitor that can be used in the research of AIDS. Saquinavir also has anti-inflammatory activity and can induce apoptosis of human red blood cells.
    Saquinavir-d<sub>9</sub>
  • HY-N7128R
    Flavanone (Standard)
    		Inhibitor
    Flavanone (Standard) is the analytical standard of Flavanone. This product is intended for research and analytical applications. Flavanone is a naturally occurring flavone. Flavanone has inhibitory activity for human estrogen synthetase (aromatase). lavanone is the inhibitor for ERK/p38/NF-κB signaling pathway. Flavanone exhibits oral activity and antitumor efficacy.
    Flavanone (Standard)
  • HY-10403A
    (aS)-PH-797804
    		Inhibitor
    (aS)-PH-797804 is a selective p38 MAPK inhibitor with IC50 values for p38 α /β of 26 nM and 102 nM, respectively. (aS)-PH-797804 has anti-inflammatory activity.
    (aS)-PH-797804
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
p38 MAPK Isoform Comparison

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