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-171301
    p38α MAPK/CK1δ inhibitor-1
    Inhibitor
    p38α MAPK/CK1δ inhibitor-1 (Compound 3) exhibits inhibitory activity against p38α MAPK and CK1δ with IC50s of 0.185 µM and 0.089 µM.
    p38α MAPK/CK1δ inhibitor-1
  • HY-171297
    p38-α MAPK-IN-10
    Inhibitor
    p38-α MAPK-IN-10 (Compound 6) is the inhibitor for p38α with an IC50 of 4 nM.
    p38-α MAPK-IN-10
  • HY-168963
    PROTAC BTK Degrader-13
    Inhibitor
    PROTAC BTK Degrader-13 (Compound 25) is the PROTAC degrader for BTK with a DC50 of 0.27 μM. PROTAC BTK Degrader-13 inhibits the activity of BTK with an IC50 of 0.44 μM, inhibits IL-2-induced T cell kinase (ITK) with an IC50 of 2.16 μM. PROTAC BTK Degrader-13 inhibits p38 MAPK signaling pathway, block the activation of the BCR (B cell receptor) signaling pathway. (Pink: ligand for target protein BTK ligand 15 (HY-168965); Black: linker (HY-Y0524); Blue: ligand for E3 ligase cereblon (HY-103596))
    PROTAC BTK Degrader-13
  • HY-175864
    EGFR-IN-173
    Inhibitor
    EGFR-IN-173 is an orally active, pan-mutant EGFR tyrosine kinase inhibitor that targets EGFR 19del, L858R/T790M and C797S triple-mutations, potently inhibiting EGFR19del/T790M/C797S with an IC50 of 1.19 nM while showing over 100-fold selectivity for mutant over wild-type EGFR (IC50 = 19.362 μM against WT). EGFR-IN-173 significantly inhibits cell migration, induces apoptosis in non-small cell lung cancer (NSCLC) cells. EGFR-IN-173 inhibits EGFR phosphorylation and suppresses the downstream pathways (MAPK/ERK, AKT, STAT3). EGFR-IN-173 exhibits antitumor efficacy in NSCLC and Ba/F3 xenograft models. EGFR-IN-173 can be used for NSCLC research.
    EGFR-IN-173
  • HY-168919
    KRASG12C IN-16
    KRASG12C IN-16 (Compound SK-17) is a selective, covalent and an orally active KRASG12C inhibitor. KRASG12C IN-16 induces Apoptosis. KRASG12C IN-16 effectively prevents the activation of MAPK and PI3K/mTOR signaling pathways. KRASG12C IN-16 displays anti-tumor activity against pancreatic cancer.
    KRASG12C IN-16
  • HY-110262
    MSC 2032964A
    Inhibitor
    MSC 2032964A is an orally active, selective inhibitor for apoptosis signal-regulating kinase 1(ASK1) with IC50 of 96 nM. MSC 2032964A preserves the visual responses in EAE mice model and exhibits potency in ameliorating the neuroinflammation.
    MSC 2032964A
  • HY-108641
    SKF-86002 dihydrochloride
    Inhibitor
    SKF-86002 dihydrochloride is an orally active p38 MAPK inhibitor, with anti-inflammatory, anti-arthritic and analgesic activities. SKF-86002 dihydrochloride inhibits lipopolysaccharide (LPS)-stimulate human monocyte IL-1 and TNF-α production (IC50 = 1 μM). SKF-86002 dihydrochloride inhibits lipoxygenase- and cyclooxygenase-mediated metabolism of arachidonic acid.
    SKF-86002 dihydrochloride
  • HY-117248
    SR-3737
    Inhibitor
    SR-3737 is a JNK3 and p38 inhibitor (IC50: 12 and 3 nM).
    SR-3737
  • HY-N1353R
    Rhamnocitrin (Standard)
    Inhibitor
    Rhamnocitrin (Standard) is the analytical standard of Rhamnocitrin. This product is intended for research and analytical applications. Rhamnocitrin is an anti-inflammatory and antioxidant agent that targets STIM-1, NFATc3 and MAPK pathways and can scavenge DPPH (IC50=28.38 mM). Rhamnocitrin selectively inhibits oxidative stress and inflammatory responses in vascular endothelial cells and neurons. Rhamnocitrin up-regulates miR-185 to inhibit STIM-1-mediated store-operated calcium entry (SOCE), thereby blocking NFATc3 nuclear translocation and downstream inflammatory factor expression, while inducing heme oxygenase HO-1 expression and regulating the ERK/p38 MAPK pathway, inhibiting antioxidant and pro-inflammatory cytokines (such as IL-6, IL-8) and adhesion molecules (such as ICAM-1, VCAM-1). Rhamnocitrin can be used in the study of endothelial-related inflammatory diseases (such as sepsis, acute lung injury, atherosclerosis) and neuroprotection (such as oxidative damage of PC12 cells).
    Rhamnocitrin (Standard)
  • HY-176740
    PROTAC Bcl-xL degrader-4
    Activator
    PROTAC Bcl-xL degrader-4 (Compound 2-38-III) is a Bcl-xL PROTAC degrader. PROTAC Bcl-xL degrader-4 has strong anti-tumor activity against HepG2 cells and HUVEC cells. PROTAC Bcl-xL degrader-4 induces cells apoptosis by decreasing mitochondrial membrane potential and activating the MAPK signaling pathway. PROTAC Bcl-xL degrader-4 significantly inhibits tumor growth in xenograft tumor mouse models. Pink: MAPK ligand (HY-176741); Blue: CRBN ligase ligand (HY-10984); Black: linker (HY-W017440)
    PROTAC Bcl-xL degrader-4
  • HY-175007
    RIPK1-IN-32
    Inhibitor
    RIPK1-IN-32 is a RIPK inhibitor with anti-inflammatory activity. RIPK1-IN-32 inhibits nitric oxide (NO) release with an IC50 of 3.26 μM. RIPK1-IN-32 significantly alleviates acute liver injury associated with sepsis through the RIPK1/NF-κB/MAPK pathway, therefore preventing the nuclear translocation of p65 and c-fos, which results in reduced expression of TNF-α and IL-6. RIPK1-IN-32 can be used for the study of acute liver injury and sepsis.
    RIPK1-IN-32
  • HY-112367
    SB 202474
    Control
    SB 202474, a negative analog of SB203580. SB 202474, which has no ability to inhibit p38 MAPK activity and is widely used as a negative control compound in p38 MAPK studies, also suppressed melanin synthesis induction.
    SB 202474
  • HY-N2420R
    Flavokawain A (Standard)
    Inhibitor
    Flavokawain A is a chalcone compound and an orally active inhibitor of PRMT5 and cytochrome P450. Flavokawain A has anti-inflammatory, anti-tumor, and immunomodulatory effects. Flavokawain A can inhibit the proliferation of tumor cells and induce apoptosis. Flavokawain A can be used in the research of diseases such as bladder cancer.
    Flavokawain A (Standard)
  • HY-N0031R
    Plantamajoside (Standard)
    Plantamajoside (Standard) is the analytical standard of Plantamajoside. This product is intended for use in research and analytical applications. Plantamajoside is an orally active phenylpropanoid glycoside. Plantamajoside can be isolated from Plantago asiatica L.(Plantaginaceae). Plantamajoside inactivates NF-κB, PI3K/akt, induces Apoptosis, and improves Autophagy. Plantamajoside regulates MAPK, integrin-linked kinase/c-Src. Plantamajoside inhibits multiple cancers, improves lung and kidney damage. Plantamajoside has neuroprotective and anti-inflammatory effects.
    Plantamajoside (Standard)
  • HY-N1965R
    Gaultherin (Standard)
    Inhibitor
    Gaultherin (Standard) is the analytical standard for Gaultherin (HY-N1965). Gaultherin is an orally active non-steroidal anti-inflammatory agent. Gaultherin selectively inhibits NF-κB, MAPK, COX-2 (IC50 = 0.35 mg/mL), LOX (IC50 = 0.56 mg/mL) and HYAL (IC50 = 28.58 μg/mL) to exert anti-inflammatory, antipyretic and analgesic effects. Gaultherin exhibits modest direct antioxidant capacity, greater in cell-based models. Gaultherin does not affect COX-1 so that avoids the common gastrointestinal side effects of Aspirin (HY-14654).
    Gaultherin (Standard)
  • HY-W744953
    Carbimazole-d3
    Inducer
    Carbimazole-d3 is deuterium labeled Carbimazole. 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-d<sub>3</sub>
  • HY-16782R
    Pexmetinib (Standard)
    Inhibitor
    Pexmetinib (Standard) is the analytical standard of Pexmetinib. This product is intended for research and analytical applications. Pexmetinib is a potent Tie-2 and p38 MAPK dual inhibitor, with IC50s of 1 nM, 35 nM and 26 nM for Tie-2, p38α and p38β, respectively, and can be used in the research of acute myeloid leukemia.
    Pexmetinib (Standard)
  • HY-10320R
    Doramapimod (Standard)
    Inhibitor
    Doramapimod (Standard) is the analytical standard of Doramapimod. This product is intended for research and analytical applications. Doramapimod (BIRB 796) is an orally active, highly potent p38 MAPK inhibitor, which has an IC50 for p38α=38 nM, for p38β=65 nM, for p38γ=200 nM, and for p38δ=520 nM. Doramapimod has picomolar affinity for p38 kinase (Kd=0.1 nM). Doramapimod also inhibits B-Raf with an IC50 of 83 nM.
    Doramapimod (Standard)
  • HY-10404A
    Dilmapimod tosylate
    Inhibitor
    Dilmapimod tosylate is a potent p38 MAPK inhibitor that potentially suppresses inflammation in chronic obstructive pulmonary disease.
    Dilmapimod tosylate
  • HY-112291A
    SB 220025 (tri(hydrochloride))
    Inhibitor
    SB 220025 trihydrochloride is a reversible, orally active, cell-permeable, ATP-competitive and selective human p38 MAPK inhibitor (IC50 = 60 nM). SB 220025 trihydrochloride also inhibits p56Lck and PKC with IC50 values of 3.5 and 2.89 μM, respectively. SB 220025 trihydrochloride inhibits the expression of IL-8 gene in response to globular adiponectin (gAd), reduces inflammatory cytokine production and inhibits angiogenesis. SB 220025 trihydrochloride effectively prevents the progression of arthritis in a chronic inflammatory disease model and can be used in the study of inflammation.
    SB 220025 (tri(hydrochloride))
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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