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Results for "

hyperphosphorylation

" in MedChemExpress (MCE) Product Catalog:

21

Inhibitors & Agonists

1

Natural
Products

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-144290
    ARN25068

    		GSK-3 DYRK Neurological Disease
    ARN25068 is a sub-micromolar inhibitor of the three protein kinases, GSK-3β, FYN and DYRK1A to tackle tau hyperphosphorylation .
    ARN25068
  • HY-151424
    Vimentin-IN-1

    		Proteasome Mitosis Cancer
    Vimentin-IN-1 is a FiVe1 derivative, an orally active and selective anticancer agent. FiVe1 binds type III intermediate filament protein vimentin (VIM), to induce hyperphosphorylation of Ser56, resulting selective disruption of mitosis and multinucleation in transformed VIM-expressing mesenchymal cancer cells. Vimentin-IN-1 shows better oral bioavailability and pharmacokinetic profiles than FiVe1 .
    Vimentin-IN-1
  • HY-139142B
    Simufilam hydrochloride
    1 Publications Verification

    PTI-125 hydrochloride

    		 mTOR iGluR Amyloid-β Tau Protein Neurological Disease
    Simufilam hydrochloride (PTI-125 hydrochloride) is an orally active FLNA modulator. Simufilam hydrochloride restores NMDAR signaling and Arc expression. Simufilam hydrochloride inhibits overactive mTOR signaling by restoring the normal conformation of FLNA, improves insulin sensitivity, reduces Aβ42-induced neuroinflammation and tau protein hyperphosphorylation. Simufilam hydrochloride can be used for research of Alzheimer's disease .
    Simufilam hydrochloride
  • HY-139142
    Simufilam
    1 Publications Verification

    PTI-125

    		 mTOR iGluR Amyloid-β Tau Protein Neurological Disease
    Simufilam (PTI-125) is an orally active FLNA modulator. Simufilam restores NMDAR signaling and Arc expression. Simufilam inhibits overactive mTOR signaling by restoring the normal conformation of FLNA, improves insulin sensitivity, reduces Aβ42-induced neuroinflammation and tau protein hyperphosphorylation. Simufilam can be used for research of Alzheimer's disease .
    Simufilam
  • HY-151873
    SZM679

    		RIP kinase Inflammation/Immunology Cancer
    SZM679 is a potent, orally active and selective RIPK1 inhibitor with Kd values of 8.6 nM and >5000 nM for RIPK1 and RIPK3, respectively. SZM679 reverses the tumor necrosis factor-induced systemic inflammatory response. SZM679 decreases the Tau hyperphosphorylation, neuroinflammation, and the RIPK1 phosphorylation level in the hippocampus and cortex. SZM679 can be used in research of Alzheimer's disease (AD) .
    SZM679
  • HY-174272
    GSK-3β inhibitor 27

    		GSK-3 Amyloid-β Neurological Disease
    GSK-3β inhibitor 27 (Compound 1c) is a reversible and competitive GSK-3β inhibitor with an IC50 value of 2.2 μM. GSK-3β inhibitor 27 inhibits tau hyperphosphorylation, reduces Aβ protein aggregation and possesses metal chelation and neuroprotective potential. GSK-3β inhibitor 27 is promising for research of neurodegenerative diseases (such as Alzheimer’s disease) .
    GSK-3β inhibitor 27
  • HY-170389
    BChE-IN-39

    		Cholinesterase (ChE) Neurological Disease
    BChE-IN-39 (Compound 7c) is a selective inhibitor for butyrylcholinesterase (BChE) with an IC50 of 0.08 μM (IC50=3.98 μM for AChE). BChE-IN-39 downregulates the GSK-3β expression, inhibits the hyperphosphorylation of tau protein .
    BChE-IN-39
  • HY-172176
    RA-PR058

    		Beta-secretase Tau Protein Neurological Disease
    RA-PR058 is an orally active Ramalin derivative with blood-brain barrier permeability, exhibiting multi-target regulatory effects and favorable pharmacokinetic properties. RA-PR058 demonstrates potential as a multi-target modulator for Alzheimer's disease by reducing the expression of BACE1, tau protein hyperphosphorylation, and anxiety-like behaviors .
    RA-PR058
  • HY-139142A
    Simufilam dihydrochloride

    PTI-125 dihydrochloride

    		 Tau Protein Amyloid-β mTOR iGluR Neurological Disease
    Simufilam dihydrochloride (PTI-125 dihydrochloride) is an orally active FLNA modulator. Simufilam dihydrochloride restores NMDAR signaling and Arc expression. Simufilam dihydrochloride inhibits overactive mTOR signaling by restoring the normal conformation of FLNA, improves insulin sensitivity, reduces Aβ42-induced neuroinflammation and tau protein hyperphosphorylation. Simufilam dihydrochloride can be used for research of Alzheimer's disease .
    Simufilam dihydrochloride
  • HY-122704
    Surfen

    Aminoquinuride

    		 FGFR HSV Tau Protein Infection Neurological Disease Inflammation/Immunology
    Surfen is a potent heparan sulfate antagonist. Surfen inhibits FGF2 binding and signal transduction. Surfen binds to glycosaminoglycans and reduces tau hyperphosphorylation. Surfen inhibits the activity of recombinant uronyl 2-O-sulfotransferase with an IC50 of approximately 2 μM. Surfen inhibits HSV-1 viral infection. Surfen inhibits neural differentiation, delays remyelination, and alleviates EAE .
    Surfen
  • HY-122704A
    Surfen dihydrochloride
    1 Publications Verification

    Aminoquinuride dihydrochloride

    		 FGFR HSV Tau Protein Infection Neurological Disease Inflammation/Immunology
    Surfen dihydrochloride is a potent heparan sulfate antagonist. Surfen inhibits FGF2 binding and signal transduction. Surfen binds to glycosaminoglycans and reduces tau hyperphosphorylation. Surfen dihydrochloride inhibits the activity of recombinant uronyl 2-O-sulfotransferase with an IC50 of approximately 2 μM. Surfen dihydrochloride inhibits HSV-1 viral infection. Surfen dihydrochloride inhibits neural differentiation, delays remyelination, and alleviates EAE .
    Surfen dihydrochloride
  • HY-124757
    FiVe1

    		Proteasome Mitosis Cancer
    FiVe1 is a vimentin (VIM) inhibitor. FiVe1 binds to the rod domain of VIM, causing metaphase VIM disassembly and hyperphosphorylation at Ser56, ultimately leading to mitotic catastrophe, multinucleation, and loss of stemness. FiVe1 has anticancer activity against soft tissue sarcomas. FiVe1 increases the sensitivity of ovarian cancer to Cisplatin (HY-17394). FiVe1 can be used for researches of mesenchymal cancers (including breast cancer and soft tissue sarcoma) and ovarian cancers .
    FiVe1
  • HY-172171
    GSK3β-IN-2

    		GSK-3 β-catenin Wnt Neurological Disease
    GSK3β-IN-2 (Compound S01) is the inhibitor for GSK3β with an IC50 of 0.35 nM. GSK3β-IN-2 activates Wnt/β-catenin signaling pathway, promotes neurogenesis and neurite growth. GSK3β-IN-2 inhibits Aβ-induced tau hyperphosphorylation at Ser396, reduces the formation of neurofibrillary tangles. GSK3β-IN-2 ameliorates Alzheimer's Disease in zebrafish model .
    GSK3β-IN-2
  • HY-136726
    CGP-82996

    CINK4

    		 CDK Cancer
    GP-82996 (CINK4) is a pharmacological inhibitor of CDK4/6. GP-82996 has IC50s of 1.5, 5.6 and 25 μM for CDK4/cyclin D1, CDK6/cyclin D1 and Cdk5/p35, respectively. GP-82996 induces the apoptosis of cancer cells U2OS. GP-82996 can be used in the research of cancer .
    CGP-82996
  • HY-149542
    GSK-3β inhibitor 15

    		Tau Protein Apoptosis GSK-3 Neurological Disease
    GSK-3β inhibitor 15 (Compound 54) is a GSK-3β inhibitor (IC50: 3.4 nM). GSK-3β inhibitor 15 inhibits Aβ1-42-induced GSK-3β and tau protein phosphorylation. GSK-3β inhibitor 15 inhibits LPS-induced iNOS expression. GSK-3β inhibitor 15 has neuroprotective effects on Aβ1-42-induced neurotoxicity. GSK-3β inhibitor 15 can be used for research of Alzheimer’s disease (AD) .
    GSK-3β inhibitor 15
  • HY-121035
    7BIO

    7-Bromoindirubin-3-Oxime

    		 CDK GSK-3 Neurological Disease
    7BIO (7-Bromoindirubin-3-Oxime) is the derivate of indirubin. 7BIO (7-Bromoindirubin-3-Oxime) has inhibitory effects against cyclin-dependent kinase-5 (CDK5) and glycogen synthase kinase-3β (GSK3β). 7BIO (7-Bromoindirubin-3-Oxime) inhibits Aβ oligomer-induced neuroinflammation, synaptic impairments, tau hyper-phosphorylation, activation of astrocytes and microglia, and attenuates Aβ oligomer-induced cognitive impairments in mice [1].
    7BIO
  • HY-173371
    BRI-50460

    		Phospholipase Neurological Disease
    BRI-50460 is an inhibitor of cytosolic calcium-dependent phospholipase A2 (cPLA2) that has the ability to penetrate the blood-brain barrier, with an IC50 of 0.88 nM. BRI-50460 exerts the activities of regulating neuroinflammation and restoring lipid homeostasis by inhibiting cPLA2, regulating the downstream inflammatory lipid signaling pathway, and alleviating the effects of amyloid β42 oligomers on the activation of cPLA2, the hyperphosphorylation of tau protein, and the reduction of synapses and dendrites. BRI-50460 can be applied to the research in the fields of Alzheimer's disease and other neurodegenerative diseases .
    BRI-50460
  • HY-139066
    Punicic acid

    Trichosanic acid

    		 TNF Receptor GLUT Proteasome Tau Protein PKC Neurological Disease Metabolic Disease Inflammation/Immunology
    Punicic acid is a bioactive compound of pomegranate seed oil. Punicic acid is an isomer of conjugated α-linolenic acid and ω-5 polyunsaturated fatty acids. Punicic acid has anti-inflammatory and antioxidant activities and can inhibit the expression of inflammatory mediators such as tumor necrosis factor α (TNF-α). Punicic acid can also reduce the formation of β-amyloid deposits and hyperphosphorylation of tau by increasing the expression of GLUT4 protein and inhibiting the overactivation of calpain, and is used to prevent and treat neurodegenerative diseases. In addition, punicic acid also has breast cancer inhibitor properties that depend on lipid peroxidation and PKC pathways .
    Punicic acid
  • HY-144316
    ZLWH-23

    		Cholinesterase (ChE) GSK-3 Neurological Disease
    ZLWH-23 is a selective AChE inhibitor (IC50=0.27 μM) with GSK-3β inhibitory property (IC50=6.78 μM). ZLWH-23 possesses selectivity for AChE over BChE (IC50=20.82 μM) and for GSK-3β over multi-kinases. ZLWH-23 has the potential for the research of Alzheimer's disease .
    ZLWH-23
  • HY-168857
    GSK-3β inhibitor 24

    		GSK-3 Tau Protein β-catenin Neurological Disease
    GSK-3β inhibitor 24 (Compound 41) is a potent GSK-3β inhibitor with an IC50 of 0.22 nM. GSK-3β inhibitor 24 increases GSK-3β phosphorylation at Ser9 site dose-dependently. GSK-3β inhibitor 24 inhibits the hyperphosphorylation of tau protein by decreasing the p-tau-Ser396 abundance. GSK-3β inhibitor 24 up-regulates β-catenin and neurogenesis-related markers (GAP43 and MAP-2). GSK-3β inhibitor 24 demonstrates remarkable anti-Alzheimer's disease (AD) effects .
    GSK-3β inhibitor 24
  • HY-162812
    H3R antagonist 4

    		Apoptosis Cholinesterase (ChE) Tau Protein Ferroptosis Histamine Receptor Neurological Disease
    H3R antagonist 4 (compound 11L) was a dual inhibitor of cholinesterase and histamine receptor (H3R), with corresponding IC50 of 7.04 μM (eeAChE), 9.73 μM (hAChE)(reversible) and 1.09 nM (H3R) , respectively. H3R antagonist 4 inhibited the aggregation of Aβ1-42 induced by itself and Cu 2+ (95.48% and 88.63%) , and degraded the Aβ1-42 fibrils induced by itself and Cu 2+ (80.16% and 89.30%) . H3R antagonist 4 chelate biometals such as Cu 2+, Zn 2+, Al 3+, and Fe 2+. H3R antagonist 4 significantly reduced tau protein hyperphosphorylation induced by Aβ1-42 and inhibited RSL-3-induced apoptosis and ferroptosis in PC12 cells. H3R antagonist 4 had the best blood-brain barrier permeability and intestinal absorption in hCMEC/D3 and hPepT1-MDCK cells.H3R antagonist 4 ameliorates learning and memory impairment in a mouse model of Alzheimer's disease induced by scopolamine (HY-N0296) .
    H3R antagonist 4

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