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-N0235
    Bakuchiol
    		Inhibitor 99.25%
    Bakuchiol is a phytoestrogen that can be obtained from psoralen seeds. Bakuchiol has been proven to be a non-competitive inhibitor of multiple enzymes, including UDP-glucuronosyltransferase 2B7 (UGT2B7) and human carboxylesterase 2 (hCE2) , with IC50s values of 40.9 μM and 7.28 μM, respectively. Bakuchiol exhibits significant research and application potential in areas such as anti-inflammatory, antibacterial, antitumor therapies, as well as drug metabolism regulation.
    Bakuchiol
  • HY-B0722
    Histamine dihydrochloride
    		Activator 99.92%
    Histamine dihydrochloride is the agonist for histamine receptor and a vasodilator. Histamine dihydrochloride is an organic nitrogen compound that participates in local immune responses, regulates intestinal physiological functions, and acts as a neurotransmitter. Histamine dihydrochloride affects p38 MAPK/Akt signaling pathway, exhibits antitumor, antioxidant and anti-inflammatory activities. Histamine dihydrochloride can be used in the research of acute myeloid leukemia, malignant melanoma, and renal cell carcinoma.
    Histamine dihydrochloride
  • HY-116522
    AR420626
    		98.29%
    AR420626 is a selective agonist of free fatty acid receptor 3 (FFAR3) (IC50=117 nM). AR420626 has anti-inflammatory, anticancer and antidiabetic activities. AR420626 improves neurogenic diarrhea by inhibiting nAChR mediated neural pathways. AR420626 inhibits the growth of HepG2 xenografts and inhibits the proliferation of hepatoma cells by inducing apoptosis. AR420626 also suppresses allergic asthma and eczema and has the ability to activate GPR41 to increase Ca2+ signal-mediated glucose uptake and improve diabetes.
    AR420626
  • HY-107427
    PF-3644022
    		Inhibitor 99.65%
    PF-3644022 is a potent, selective, orally active and ATP-competitive MAPKAPK2 (MK2) inhibitor with an IC50 of 5.2 nM and a Ki of 3 nM. PF-3644022 also inhibits MK3 and p38 regulated/activated kinase (PRAK) with IC50s of 53 nM and 5.0 nM, respectively. PF-3644022 potently inhibits TNFα production and has anti-inflammatory effect.
    PF-3644022
  • HY-P99386
    Vesencumab
    		Inhibitor 99.34%
    Vesencumab (MNRP-1685A) is IG1 antibody against neuropilin-1 (NRP-1). Vesencumab binds to NRP-1 and prevents the subsequent coupling of NRP-1 to VEGFR-2. Vesencumab has anti-angiogenic and anti-neoplastic activities. Vesencumab can be used in the research of metastatic solid tumors, including ovarian cancer.
    Vesencumab
  • HY-P1178
    Cyclotraxin B
    		Inhibitor 99.78%
    Cyclotraxin B is a BBB-penetrable and selective TrkB inhibitor. Cyclotraxin B inhibits BDNF-induced TrkB activity in a non-competitive manner, with an IC50 of 0.30 nM. Cyclotraxin B has analgesic and anxiolytic effects.
    Cyclotraxin B
  • HY-10295A
    SB 202190 hydrochloride
    		Inhibitor 99.66%
    SB 202190 hydrochloride is a selective p38 MAP kinase inhibitor with IC50s of 50 nM and 100 nM for p38α and p38β2, respectively. SB 202190 hydrochloride binds to the ATP pocket of the active recombinant human p38 kinase with a Kd of 38 nM. SB 202190 hydrochloride has anti-cancer activity. SB202190 hydrochloride induces autophagy.
    SB 202190 hydrochloride
  • HY-10403
    PH-797804
    		Inhibitor 98.94%
    PH-797804 is a ATP-competitive, selective p38α/p38β inhibitor (IC50=26 nM and Ki=5.8 nM for p38α; Ki=40 nM for p38β) and does not inhibit JNK2.
    PH-797804
  • HY-17003
    Saquinavir mesylate
    		Inhibitor 99.84%
    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
  • HY-12839
    p38 MAPK-IN-1
    		Inhibitor 99.58%
    p38 MAPK-IN-1 (Compound 4) is a novel potent and selective inhibitor of p38 MAPK with IC50 of 68 nM. p38 MAPK-IN-1 shows sustained levels, low clearance and good bioavailability.
    p38 MAPK-IN-1
  • HY-B0435
    Roxithromycin
    		Activator 99.86%
    Roxithromycin (RU-28965) is an orally active semi-synthethic macrolide antibiotic. Roxithromycin inhibits protein biosynthesis in the elongation step by binding to 50S bacterial ribosome. Roxithromycin has antimicrobial, antiproliferative, anti-inflammatory, tumour vasculature inhibiting and lung injury ameliorating effects.
    Roxithromycin
  • HY-10021
    Varenicline Tartrate
    		Activator 99.96%
    Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50 = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α6β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation.
    Varenicline Tartrate
  • HY-11068
    SB 239063
    		Inhibitor 99.49%
    SB 239063 is a potent, selective and orally active p38 MAPK inhibitor, exhibits an IC50 of 44 nM for recombinant purified human p38α, with equipotent inhibitory activity against p38α and p38β. SB 239063 has no effect on p38γ or p38δ. With anti-asthma activity and also be used to enhance memory which is impaired due to aging or medical conditions, such as, AD.
    SB 239063
  • HY-A0033
    Darifenacin
    		Inhibitor 99.81%
    Darifenacin (UK-88525) is a selective and orally active M3 muscarinic receptor (M3R) antagonist with a pKi of 8.9. Darifenacin binds >20-fold more specifically to M3R than to other muscarinic receptors. Darifenacin can be used in the study of urinary incontinence and other symptoms of overactive bladder. Darifenacin inhibits tumor growth in colorectal cancer cells and has anti-tumor effects.
    Darifenacin
  • HY-119272
    EF24
    		Inhibitor 99.34%
    EF24, a curcumin analogue, is an NF-kB inhibitor with great anti-tumor efficacy and oral bioavailability via deactivation of the MAPK/ERK signaling pathway in oral squamous cell carcinoma (OSCC). EF24 is active against melanoma and breast cancer cell lines with GI50 values of 0.7 μM and 0.8 μM, respectively. EF24 induces cell cycle arrest and apoptosis in MDA-MB-231 human breast cancer cells and DU-145 human prostate cancer cells. EF24 increases the levels of activated caspase 3 and 9, and decreases the phosphorylated forms of MEK1 and ERK.
    EF24
  • HY-110313
    SB-747651A dihydrochloride
    		Inhibitor 99.14%
    SB-747651A dihydrochloride is an ATP-competitive mitogen- and stress-activated kinase 1 (MSK1) inhibitor with an IC50 of 11 nM. SB-747651A dihydrochloride also inhibits PRK2, RSK1, p70S6K and ROCK-II. SB-747651A dihydrochloride can be used for inflammation research.
    SB-747651A dihydrochloride
  • HY-124284
    Hexamethylene bisacetamide
    		Inhibitor 99.56%
    Hexamethylene bisacetamide (HMBA) is a differentiation inducer and selective bromine domain inhibitor that can differentiate across the blood-brain barrier. Hexamethylene bisacetamide can induce tumor cell differentiation and inhibit cell proliferation, showing antitumor activity. Hexamethylene bisacetamide induces apoptosis by Notch1, Bcl-2 and p53 signaling pathways. In addition, Hexamethylene bisacetamide improves the obesity phenotype of mice.
    Hexamethylene bisacetamide
  • HY-10406
    Talmapimod
    		Inhibitor 98.68%
    Talmapimod (SCIO-469) is an orally active, selective, and ATP-competitive p38α inhibitor with an IC50 of 9 nM. Talmapimod shows about 10-fold selectivity over p38β, and at least 2000-fold selectivity over a panel of 20 other kinases, including other MAPKs.
    Talmapimod
  • HY-14806B
    Teneligliptin hydrobromide hydrate
    		Inhibitor 99.97%
    Teneligliptin (MP-513) hydrobromide hydrate is an orally active and selective dipeptidyl peptidase 4 (DPP-4) inhibitor (IC50s: 0.37 and 0.29 nM for the human and rat DPP-4, respectively). Teneligliptin hydrobromide hydrate improves blood glucose levels and can be used in researches related to type 2 diabetes mellitus.
    Teneligliptin hydrobromide hydrate
  • HY-N0763
    Angelicin
    		Inhibitor 99.98%
    Angelicin is a furanocoumarin compound that functions as an inhibitor of NF-κB and MAPK signaling pathways, exhibiting anti-inflammatory, antiviral, and antitumor activities. It suppresses the lytic replication of γ-herpesviruses, such as MHV-68, early during viral infection, potentially inhibiting RTA gene expression (IC50=28.95 μM). Angelicin also mitigates inflammation by inhibiting the phosphorylation and nuclear translocation of NF-κB, and the phosphorylation of p38 and JNK. Furthermore, it induces apoptosis in neuroblastoma cells by downregulating anti-apoptotic proteins like Bcl-2, Bcl-xL, and Mcl-1, while activating caspase-9 and caspase-3.
    Angelicin
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
p38 MAPK Isoform Comparison

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