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-108645
    AL 8697
    		Inhibitor 99.92%
    AL 8697 is a specific and orally active p38α MAPK inhibitor with an IC50 of 6 nM. AL 8697 displays 14-fold greater inhibition of p38α compared to p38β (IC50=82 nM), and 300-fold selectivity for p38α over a panel of 91 kinases. Anti-inflammatory activity.
    AL 8697
  • HY-N7085R
    Citropten (Standard)
    		Inhibitor
    Citropten (Standard) is the analytical standard of Citropten. This product is intended for research and analytical applications. Citropten (5, 7-dimethoxycoumarin) is one of the coumarin derivatives. Citropten is an effective oral anticancer agent. Citropten has anti-proliferative activity against A2058 and B16 melanoma cells. Citropten exerts anti-inflammatory effects through the NFκB and MAPK signaling pathways. Citropten acts as an antidepressant through heat shock protein-70, monoamine oxidase-A and inhibition of apoptosis .
    Citropten (Standard)
  • HY-Y1322S
    Triphenyl phosphate-d15
    		Inhibitor 99.74%
    Triphenyl phosphate-d15 is the deuterium labeled Triphenyl phosphate. Triphenyl phosphate is an orally active, blood-brain barrier-permeable aryl organophosphate flame retardant and endocrine disruptor. Triphenyl phosphate disrupts mitochondrial dynamic balance through oxidative stress, induces excessive mitophagy and apoptosis, and ultimately leads to myocardial fibrosis. In the brain, Triphenyl phosphate activates the NF-κB inflammatory pathway by disrupting the gut microbiota, alters tryptophan metabolism and elevates neurotoxins, thereby inducing anxiety- and depression-like behaviors. In the skeletal and reproductive systems, Triphenyl phosphate inhibits osteoblast differentiation and induces germ cell apoptosis by suppressing the MAPK/ERK pathway and activating the JNK signal, respectively. In adipose and placental tissues, Triphenyl phosphate promotes lipid accumulation by activating the PI3K/AKT-PPARγ axis, and disrupts placental metabolism via the MAOA/ROS/NF-κB cascade, impairing neurodevelopment of offspring.
    Triphenyl phosphate-d<sub>15</sub>
  • HY-120349
    LL-Z1640-4
    		Inhibitor 99.0%
    LL-Z1640-4 is a potent p38/JNK signaling inhibitor. LL-Z1640-4 significantly diminishes p38 and JNK activation in HCC cells transfected with MLK4 siRNA. LL-Z1640-4 markedly attenuates ROS production induced by MLK4 knockdown. LL-Z1640-4 significantly reduces the apoptotic cells in HCC cells transfected with siMLK4.
    LL-Z1640-4
  • HY-114405
    SJFδ
    		Inhibitor
    SJFδ is a 10-atom linker PROTAC based on von Hippel-Lindau ligand. SJFδ degrades p38δ with a DC50 of 46.17 nM, but does not degrade p38α, p38β, or p38γ.
    SJFδ
  • HY-28325
    AMC-04
    		Inducer 98.48%
    AMC-04 is an unfolded protein response (UPR) activator, which activates UPR pathway through ROS and p38 MAPK signaling and induces apoptotic cell death. AMC-04 can be used for cancer research.
    AMC-04
  • HY-N0188R
    Esculin (Standard)
    		Inhibitor
    Esculin (Standard) is the analytical standard of Esculin. This product is intended for research and analytical applications. Esculin is a fluorescent coumarin glucoside, the active ingredient in ash bark. Esculin has antidiabetic effects, improves cognitive impairment in experimental diabetic nephropathy (DN) via the MAPK signaling pathway, and exerts antioxidant stress and anti-inflammatory effects. Esculin also has anticancer, antibacterial, antiviral, neuroprotective, antithrombotic, and therapeutic properties for eye diseases.
    Esculin (Standard)
  • HY-P6084
    RP-220
    		Activator
    RP-220 is a renalase peptide targeting NLRP3. RP220 has anti-inflammatory and anti-apoptotic activities. RP220 inhibits renal tubular epithelial cells apoptosis with alkaline insult by activating MAPK signaling pathway. RP220 significantly inhibits NLRP3 expression and reduces macrophage infiltration and kidney tissue damage in acute kidney injury (AKI) mice model. RP-220 can be uses for systemic lupus erythematosus (SLE) and its complication lupus nephritis (LN) research.
    RP-220
  • HY-N2192
    Swertianolin
    		Inhibitor 99.54%
    Swertianolin is a xanthone glycoside. Swertianolin can be isolated from plants of the Gentianaceae family (e.g., Gentiana campestris and Swertia punicea). Swertianolin inhibits p38 phosphorylation and NF-κB activation, and reduces NO and ROS production. Swertianolin exhibits anti-Helicobacter pylori activity with an IC50 of 6.1 μM and a minimum bactericidal concentration of 91.7 μM. Swertianolin modulates immune function in sepsis. Swertianolin is useful in the research of diseases such as Alzheimer's disease, hepatitis B, Helicobacter pylori infection, and sepsis.
    Swertianolin
  • HY-N6651
    Isocryptotanshinone
    		Activator ≥98.0%
    Isocryptotanshinone is a dual STAT3 and PTP1B (IC50 = 56.1 μM) inhibitor. Isocryptotanshinone inhibits STAT3 by binding to the STAT3 SH2 domain to block phosphorylation and nuclear translocation[1][2]. Isocryptotanshinone exerts its anti-proliferative effect via the induction of cell cycle arrest, apoptosis, and pro-death autophagy, through the regulation of STAT3, AKT/mTOR and MAPK signaling pathways. Isocryptotanshinone suppresses the xenograft gastric cancer (GC) tumor growth in BALB/c nude mice. Isocryptotanshinone can be used for cancer research, such as lung cancer, breast cancer and GC.
    Isocryptotanshinone
  • HY-143212
    18:0-22:6 DG
    		Modulator 99%
    18:0-22:6 DG (1-Stearoyl-2-docosahexaenoyl-sn-glycerol) is a diacylglycerol (DG) that can interact with RasGRP (Ras guanine nucleotide-releasing protein) (Ki = 8.37 μM) and modulate the activation of MAP kinases (such as ERK1/ERK2), which play a crucial role in cellular signaling processes. 18:0-22:6 DG can also activate protein kinase C (PKC) isozyme. 18:0-22:6 DG can be used for research of cancer, immunology and metabolic disease.
    18:0-22:6 DG
  • HY-N1365R
    Isoscopoletin (Standard)
    		Inhibitor
    Isoscopoletin (Standard) is the analytical standard of Isoscopoletin. This product is intended for research and analytical applications. Isoscopoletin (6-Hydroxy-7-methoxycoumarin) is an active constituent in Artemisia argyi leaves. Isoscopoletin shows substantial inhibition against cell proliferation, with IC50s of 4.0 μM and 1.6 μM for human CCRF-CEM leukaemia cells and multidrug resistant subline CEM/ADR5000, respectively. Isoscopoletin (6-Hydroxy-7-methoxycoumarin) possesses inhibitory activity against HBV replication. Isoscopoletin exhibits anti-inflammatory activity through inhibition of MAPK/NF-κB/STAT/AKT signaling pathway.
    Isoscopoletin (Standard)
  • HY-145564A
    Emprumapimod hydrochloride
    		Inhibitor 98.0%
    Emprumapimod (PF-07265803) hydrochloride is an orally active and selective inhibitor of p38α MAPK. Emprumapimod hydrochloride can be used for the research of dilated cardiomyopathy and acute inflammatory pain.
    Emprumapimod hydrochloride
  • HY-N0430
    Coptisine
    		Inhibitor
    Coptisine is an orally active and brain-penetrant alkaloid found in Coptis chinensis. Coptisine is a reversible, uncompetitive IDO inhibitor with a Ki of 5.8 μM and an IC50 of 6.3 μM. Coptisine suppresses neuroinflammation, reduces Aβ plaque burden and shows neuroprotective activity. Coptisine shows anti-inflammation activity by blocking NF-κB, MAPK, and PI3K/Akt activation. Coptisine inhibits cancer cells proliferation, induces DNA damage, G2/M phase cell cycle arrest, apoptosis, ROS production and mitochondrial dysfunction. Coptisine inhibits Rho/ROCK pathway activation, reduces arrhythmia, limits cardiac injury marker release, reduces infarct size, and preserves cardiac function in rat myocardial ischemia/reperfusion models. Coptisine downregulates HMGCR and upregulates LDLR and CYP7A1 to modulate cholesterol metabolism, reduces abnormal serum lipid levels, and promotes fecal bile acid excretion. Coptisine can be used for the research of cancer, hypercholesterolemia, Alzheimer’s disease, inflammatory disorders and cardiovascular disease.
    Coptisine
  • HY-175703
    RANKL-IN-1
    		Inhibitor
    RANKL-IN-1 is a selective and orally active Receptor Activator of Nuclear Factor-κ B Ligand (RANKL) inhibitor with a KD value of 7.6 μM. RANKL-IN-1 exhibits inhibitory activity and selectivity against osteoclastogenesis with an IC50 value of 0.07 μM and SI of 82.57. RANKL-IN-1binds directly to RANKL and blocks the RANKL-induced activation of the NF-κB and MAPK pathways. RANKL-IN-1 can be used for the research of metabolic disease, such as osteoporosis.
    RANKL-IN-1
  • HY-N2199
    Sotetsuflavone
    		Inhibitor
    Sotetsuflavone is a flavonoid that can be isolated from Cycas revolute. Sotetsuflavone inhibits phosphorylation of PI3K, Akt, mTOR, JNK, and p38 MAPK; modulates expression of Cyclin D1, CDK4, Bcl-2, Bax, cleaved caspases 3/9, MMP-9, TGF-β, STAT3, and β-catenin. Sotetsuflavone induces G0/G1 cell cycle arrest, apoptosis, autophagy, and intracellular ROS elevation, inhibits cancer cell proliferation. Sotetsuflavone inhibits tumor growth in mouse tumor xenograft models. Sotetsuflavone can be used for the research of non-small cell lung cancer and Crohn’s disease.
    Sotetsuflavone
  • HY-18754A
    FR 167653
    		Inhibitor 99.87%
    FR 167653 (FR 167653 sulfate), an orally active and selective p38 MAPK inhibitor, is a potent suppressor of TNF-α and IL-1β production via specific inhibition of p38 MAPK activity. FR 167653 (FR 167653 sulfate) is effective in treating inflammation, relieving trauma and ischemia-reperfusion injury in vivo.
    FR 167653
  • HY-159798
    NR-11c
    		Inhibitor 99.75%
    NR-11c is a selective and potent p38α PROTAC degrader. NR-11c effectively degrades p38α in a variety of tumor cells. When administered intraperitoneally or intravenously to mice, NR-11c primarily acts in the liver. NR-11c can be used in cancer research. (Pink: p38α inhibitor 5 (HY-159799); Black: linker (HY-159800); Blue: VHL E3 ligase ligand (HY-112078)).
    NR-11c
  • HY-179095
    UR241-2
    		Inhibitor 99.68%
    UR241-2 is an IRAK4 inhibitor. UR241-2 suppresses IL-1–induced IRAK1/4 signaling, NF-κβ activation, and phosphorylation of p65 and p38. UR241-2 selectively inhibits leukemia stem cell clonogenicity. UR241-2 can serve as a ligand for target proteins for PROTAC, facilitating the development and design of PROTAC degraders for IRAK4. UR241-2 can be used in the research of acute myeloid leukemia.
    UR241-2
  • HY-120967A
    (2S)-OMPT
    (2S)-OMPT, Lysophosphatidic acid analogue, is a LPA3 G-protein-coupled receptor agonist. (2S)-OMPT selectively activates LPA3 G-protein-coupled receptor to trigger downstream cellular signaling events. (2S)-OMPT induces calcium, IL-6 release in cancer cells and activates MAPK and Akt signaling pathways. (2S)-OMPT can be used for the research of ovarian cancer.
    (2S)-OMPT
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
p38 MAPK Isoform Comparison

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