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-13468A
    KW-2478 hydrochloride
    		Inhibitor
    KW-2478 hydrochloride is an HSP90 inhibitor (IC50 = 3.8 nM). KW-2478 hydrochloride inhibits the growth and induces apoptosis in chronic myeloid leukemia (CML) cells and liver cancer cells. KW-2478 hydrochloride weakens the BCR/ABL and MAPK signaling pathways, leading to increased p27 and p21 expression and decreased cyclin B1 expression. KW-2478 hydrochloride downregulates STAT3 expression. KW-2478 hydrochloride may be used in research on cancers such as CML and liver cancer.
    KW-2478 hydrochloride
  • HY-178391
    SMU-037
    		Inhibitor
    SMU-037 is an orally active and selective ROS1 inhibitor that demonstrates potent activity (IC₅₀ = 6.8 nM) and possesses the ability to penetrate the blood-brain barrier. SMU-037 shows ~25-fold selectivity over ALK, and superior sensitivity against the G2032R mutation. SMU-037 attenuates phosphorylation of ROS1 and downstream MAPK-ERK signaling pathway, leading to cell cycle arrest and apoptosis. SMU-037 effectively suppresses tumor progression in both xenograft and intracranial mouse models. SMU-037 can be used for non-small cell lung cancer (NSCLC) research.
    SMU-037
  • HY-17003R
    Saquinavir mesylate (Standard)
    		Inhibitor
    Saquinavir mesylate (Standard) (Ro 31-8959/003 (Standard)) is the analytical standard of Saquinavir mesylate (HY-17003). This product is intended for research and analytical applications. Saquinavir (Ro 31-8959) mesylate is an orally active HIV protease inhibitor that can be used in the research of AIDS. Saquinavir mesylate also has anti-inflammatory activity and can induce apoptosis of human red blood cells.
    Saquinavir mesylate (Standard)
  • HY-10320G
    Doramapimod (GMP)
    		Inhibitor
    Doramapimod GMP (BIRB 796 GMP) is an orally active inhibitor for p38 MAPK, with IC50s of 38, 65, 200 and 520 nM, for p38α, p38β, p38γ, p38δ. Doramapimod exhibits cytotoxicity and antitumor activity against multiple myeloma, synergizes with multidrug resistance protein 1 (ABCB1) and aurora kinase inhibitor VX680, promoting their antitumor efficacy against oral epidermoid carcinoma and cervical cancer. Doramapimod also exhibits anti-inflammatory activity.
    Doramapimod (GMP)
  • HY-174437B
    FLT3-IN-32 hydrochloride
    		Inhibitor
    FLT3-IN-32 hydrochloride is a potent and orally active FLT3 inhibitor with an IC50s of 0.29 nM, 0.77 nM and 2.07 nM against FLT3-ITD, FLT3-D835Y and FLT-N676K. FLT3-IN-32 hydrochloride reduces the phosphorylation of FLT3 and its downstream signaling molecules (STAT5, MAPK, AKT) to induce FLT3-mutated Ba/F3 cells apoptosis. FLT3-IN-32 hydrochloride shows significant anti-tumor efficacy in n the MV4-11 xenograft model. FLT3-IN-32 hydrochloride can be used for the study of acute myeloid leukemia (AML).
    FLT3-IN-32 hydrochloride
  • HY-P5641
    Pleurocidin
    		Inhibitor 98.91%
    Pleurocidin is an Antimicrobial peptide. Pleurocidin is derived from the skin mucosa or intestinal secretions of Pseudopleuronectes americanus. Pleurocidin inhibits the expression of key proteins in the MAPK and NF-κB inflammatory signaling pathways. Pleurocidin alters serum inflammatory and immune cytokine levels, regulates the down-regulation of tight junction proteins, and modulates the intestinal flora. Pleurocidin exerts antibacterial activity by inducing bacterial membrane damage, hydroxyl radical formation, and NADH depletion, and also produces a synergistic effect with Antibiotics. Pleurocidin alleviates DSS-induced ulcerative colitis. Pleurocidin can be used for research on ulcerative colitis, bacterial infections, and bacterial biofilm-related infections.
    Pleurocidin
  • HY-183936
    SDUY127
    		Inhibitor
    SDUY127 is a bivalent SHP2 inhibitor with an IC50 value of 16 nM. SDUY127 binds simultaneously to the tunnel allosteric site and latch allosteric site of SHP2 at a 1:1 stoichiometric ratio, stabilizes the protein in an inactive conformation, and induces sustained inhibition of the MAPK signaling pathway. SDUY127 can be used in research related to leukemia and hepatocellular carcinoma.
    SDUY127
  • HY-10261AR
    Afatinib dimaleate (Standard)
    		Inhibitor
    Afatinib (dimaleate) (Standard) is the analytical standard of Afatinib (dimaleate). This product is intended for research and analytical applications. Afatinib (BIBW 2992) dimaleate 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 dimaleate can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer.
    Afatinib dimaleate (Standard)
  • HY-N17317
    Isostrictiniin
    		Inhibitor
    Isostrictiniin (ITN) is a polyphenolic compound isolated from Nymphaea candida. It upregulates the expression of Nrf2 and HO-1, while downregulating the expression of Keap1. Isostrictiniin reduces the phosphorylation levels of JNK, ERK1/2, p38, IκBα, and NF-κB p65. Isostrictiniin decreases the levels of pro-inflammatory mediators (IL-1β, IL-6, TNF-α, PGE2). Isostrictiniin alleviates LPS-induced acute lung injury and exerts protective effects against acute alcoholic liver injury. Additionally, isostrictiniin exhibits anti-inflammatory, antioxidant, and anti-fibrotic activities.
    Isostrictiniin
  • HY-114422
    ARRY-371797
    		Inhibitor
    ARRY-371797 is a potent and orally active p38α MAPK and BChE inhibitor with IC50 values of 12.0, 0.13, ＞100 µM for p38α MAP, hBChE, hAChE, respectively. ARRY-371797 has the potential for the research of Alzheimer’s disease.
    ARRY-371797
  • HY-12716
    BRL-44408
    		Inhibitor
    BRL-44408 is a selective, blood-brain barrier-permeable α2A-adrenergic receptor antagonist with a Ki value of 8.56 nM against human targets. BRL-44408 exhibits activities such as antidepressant, analgesic effects and attenuation of sepsis-induced acute lung injury by regulating the release of neurotransmitters such as norepinephrine and dopamine, or inhibiting signaling pathways including ERK1/2, p38MAPK and p65. BRL-44408 can be used in studies related to acute respiratory distress syndrome, depression and visceral pain.
    BRL-44408
  • HY-168482
    NF-κB/MAPK-IN-2
    		Inhibitor
    NF-κB/MAPK-IN-2 (compound 14) is a potent NF-κB and MAPK Inhibitor. NF-κB/MAPK-IN-2 decreases the protein expression of p-p65, p-IκB, p-p38, p-JNK, and p-ERK. NF-κB/MAPK-IN-2 reduces the LPS-induced release of TNF-α and IL-6. NF-κB/MAPK-IN-2 inhibits nuclear translocation of p65 and c-Fos. NF-κB/MAPK-IN-2 has the potential for the research of sepsis.
    NF-κB/MAPK-IN-2
  • HY-120505
    ITZ-1
    		Inhibitor
    ITZ-1 is an orally active and selective extracellular signal-regulated kinase (ERK)-mitogen-activated protein kinase (MAPK) pathway inhibitor with an IC50 of 0.51 μM for inhibiting interleukin-1β (IL-1β)-induced matrix metalloproteinase-13 (MMP-13) production. ITZ-1 reduces MMP-13 expression and suppresses nitric oxide (NO)-induced chondrocyte apoptosi. ITZ-1 is promising for research of osteoarticular diseases.
    ITZ-1
  • HY-175971
    PDE1-IN-10
    		Inhibitor
    PDE1-IN-10 is a potent and sekective Phosphodiesterase 1 (PDE1) inhibitor with an IC50 of 5 nM. PDE1-IN-10 can suppress TGF-β/Smad-MAPK signaling and exhibit antifibrotic effects. PDE1-IN-10 can be used for the research of idiopathic pulmonary fibrosis.
    PDE1-IN-10
  • HY-10261E
    (R)-Afatinib
    		Inhibitor
    (R)-Afatinib ((R)-BIBW 2992) is the Afatinib isomer. Afatinib (HY-10261) 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.
    (R)-Afatinib
  • HY-107272
    Chuanbeinone
    		Inhibitor
    Chuanbeinone (22-Epidelavinone) is an orally active alkaloid found in Fritillaria pallidiflora. Chuanbeinone shows cytotoxicity against mutiple cancer cells and can induces apoptosis and S phase arrest. Chuanbeinone downregulates Bcl-2, upregulates Bax, and activates caspase-3. Chuanbeinone exerts anti-inflammatory and antitussive effects by reducing pro-inflammatory cytokine (IL-1β, IL-6 and TNF-α) production and mRNA expression, and inhibiting TRIF-, MyD88-, NF-κB-, and MAPK-dependent signaling pathways. Chuanbeinone inhibits AChE and BChE with IC50 values of 7.7 and 0.7 μM. Chuanbeinone can be used for the researches of lung carcinoma, cough, inflammatory diseases.
    Chuanbeinone
  • HY-183365
    SL43
    		Inhibitor
    SL43 is an orally active and potent SOS1 inhibitor with a Kd of 0.16 μM. SL43 disrupts SOS1-KRAS interaction, inhibits SOS1-mediated nucleotide exchange on KRAS mutants, and suppresses RAS-MAPK signaling. SL43 exerts antiproliferative activity against KRAS-mutant cancer cells, induces early apoptosis and G1 phase cell cycle arrest, and reduces phosphorylated MEK and ERK levels. SL43 suppresses tumor growth in a colorectal cancer xenograft model.
    SL43
  • HY-151921
    Anti-inflammatory agent 33
    		Inhibitor
    Anti-inflammatory agent 33 is a potent p38α inhibitor. Anti-inflammatory agent 33 inhibits NO production. Anti-inflammatory agent 33 inhibits LPS-induced iNOS, COX-2, p-p38α, p-MK2 protein expression. Anti-inflammatory agent 33 shows anti-inflammatory activity.
    Anti-inflammatory agent 33
  • HY-180336
    LM9
    		Inhibitor
    LM9 is a potent, orally active MyD88 inhibitor. LM9 blocks TLR4/MyD88 binding, MyD88 homodimer formation, and TLR4/MyD88/NF-κB signaling pathway activation. LM9 prevents atherosclerosis by regulating inflammatory responses and oxidative stress in macrophages. LM9 efficiently mitigates inflammatory responses and fibrosis in obesity-induced cardiomyopathy. LM9 can be used for fibrosis and atherosclerosis research.
    LM9
  • HY-180807
    MAPK-IN-6
    		Inhibitor
    MAPK-IN-6 (compound 116B) is a CNS-penetrant compound that inhibits the MAPK signaling pathway. MAPK-IN-6 reduces oxidative stress in SH-SY5Y neuronal cells by reducing ROS, restoring mitochondrial function, and inhibiting MAPK-driven inflammation. MAPK-IN-6 demonstrates profound neuroprotective efficacy in a rat tBCCAO/R model via ERK-P38-JNK signaling. MAPK-IN-6 can be used as a neuroprotective agent in ischemic stroke research.
    MAPK-IN-6
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
p38 MAPK Isoform Comparison

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