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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
20 Results for "
Tau protein hyperphosphorylation
" in MedChemExpress (MCE) Product Catalog:
Products (20)
20 Results for "Tau protein hyperphosphorylation" in MCE Product Catalog:
1
Target:
Research Areas:
Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
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 .
1
1 Cited Publications
Synonyms: Trichosanic acid
Category:
Punica granatum L. Ketones, Aldehydes, Acids Metabolic Disease Punicaceae Plants Disease Research Fields
Target:
1
1 Cited Publications
Cat. No.: HY-N0695
CAS No.: 58546-55-7
Synonyms: Gomisin-B; Wuweizi ester-B; Schisantherin-B
1
1 Cited Publications
Synonyms: Hexahydroadiphenine hydrochloride
Target:
Cholinesterase (ChE) Potassium Channel Amyloid-β TRP Channel Tau Protein NOD-like Receptor (NLR) JNK NF-κB IKK
Research Areas:
Neurological Disease Metabolic Disease Inflammation/Immunology
Drofenine (Cycloadiphene; Hexahydroadiphenine) hydrochloride is an brain-penetrant antispasmodic agent. Drofenine hydrochloride is a Kv2.1 channel inhibitor with human IC50 of 9.53 μM. Drofenine hydrochloride is a butyrylcholinesterase (BChE) inhibitor with Ki of 0.003 mM, and is a TRPV3 activator. Drofenine hydrochloride blocks Kv2.1-dependent potassium efflux, inhibits Kv2.1/JNK/NF-κB and IkBa/NF-kB signaling, suppresses Kv2.1 mRNA/protein expression. Drofenine suppresses oligomeric Aβ-induced microglial NLRP3 inflammasome activation and neuronal Tau hyperphosphorylation, improves cognitive impairment, promotes neurite outgrowth. Drofenine hydrochloride induces calcium influx in keratinocytes and exert cytotoxicity against keratinocytes. Drofenine hydrochloride ameliorates diabetic peripheral neuropathy -like pathology. Drofenine hydrochloride can be used for the researches of Alzheimer's disease, diabetic peripheral neuropathy and smooth muscle spasm .
1
1 Cited Publications
Synonyms: PTI-125 hydrochloride
Target:
Research Areas:
Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
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 .
Target:
Research Areas:
CS640 (Compound 19) is a chemical probe and a calmodulin-dependent kinase inhibitor. CS640 inhibits CaMK1D, CaMK1B, CaMK1A, CaMK1G, MEK5, RIPK4, mLK3 and PIP5K1, with IC50 values of 8, 3, 1, 1, 25 nM, 5.69, 2.75 and 11.2 μM, respectively. CS640 blocks Aβ-induced hyperphosphorylation of tau protein at the Thr181 site, but fails to protect primary mouse cortical neurons from Aβ-induced toxic damage. CS640 is applicable to research related to Alzheimer's disease .
Research Areas:
ARN25068 is a sub-micromolar inhibitor of the three protein kinases, GSK-3β, FYN and DYRK1A to tackle tau hyperphosphorylation .
Cat. No.: HY-173371
Target:
Research Areas:
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 .
Cat. No.: HY-139142A
CAS No.: 2480226-06-8
Synonyms: PTI-125 dihydrochloride
Target:
Research Areas:
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 .
Cat. No.: HY-168857
CAS No.: 3069913-37-4
Target:
Research Areas:
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 .
Cat. No.: HY-174272
Research Areas:
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) .
Cat. No.: HY-175841
CAS No.: 3075165-36-2
Target:
Research Areas:
Tau Protein Phosphorylation-IN-1 is a tau protein phosphorylation inhibitor that potently protects PC12 cells against Aβ25–35-induced cytotoxicity (EC50 = 1.93 μM), and can penetrate the blood-brain barrier (BBB).Tau Protein Phosphorylation-IN-1 reverses the hyperphosphorylation of tau, significantly inhibits the expression of certain immune-related cytotoxic factors, suppresses the MAPK and NF-κB signaling pathways, and significantly inhibits the expression of RAGE and the apoptosis factors Bax/Bcl-2, both in vitro and in vivo. Tau Protein Phosphorylation-IN-1 relieves nerve damage, and improves learning and memory in an Alzheimer’s disease (AD) mouse model. Tau Protein Phosphorylation-IN-1 can be used for AD research .
Cat. No.: HY-170389
Target:
Research Areas:
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 .
Cat. No.: HY-172176
Target:
Research Areas:
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 .
Cat. No.: HY-N0695R
CAS No.: 58546-55-7
Synonyms: Gomisin-B (Standard); Wuweizi ester-B (Standard); Schisantherin-B (Standard)
Target:
Potassium Channel Cholinesterase (ChE) TRP Channel NOD-like Receptor (NLR) Amyloid-β Tau Protein JNK NF-κB IKK
Research Areas:
Neurological Disease Metabolic Disease Inflammation/Immunology
Drofenine (Cycloadiphene; Hexahydroadiphenine) is an brain-penetrant antispasmodic agent. Drofenine is a Kv2.1 channel inhibitor with human IC50 of 9.53 μM. Drofenine is a butyrylcholinesterase (BChE) inhibitor with Ki of 0.003 mM, and is a TRPV3 activator. Drofenine blocks Kv2.1-dependent potassium efflux, inhibits Kv2.1/JNK/NF-κB and IkBa/NF-kB signaling, suppresses Kv2.1 mRNA/protein expression. Drofenine suppresses oligomeric Aβ-induced microglial NLRP3 inflammasome activation and neuronal Tau hyperphosphorylation, improves cognitive impairment, promotes neurite outgrowth. Drofenine induces calcium influx in keratinocytes and exert cytotoxicity against keratinocytes. Drofenine ameliorates diabetic peripheral neuropathy -like pathology. Drofenine can be used for the researches of Alzheimer's disease, diabetic peripheral neuropathy and smooth muscle spasm .
Cat. No.: HY-162812
Research Areas:
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) .
Cat. No.: HY-184078
CAS No.: 1563106-65-9
Research Areas:
8-F-2-(Me-Pip-Me)-Tryptanthrin is a tryptanthrin derivative with blood-brain barrier penetration. 8-F-2-(Me-Pip-Me)-Tryptanthrin protects neurons from Aβ-induced apoptosis, inhibits Aβ-induced Tau protein hyperphosphorylation and neuronal synaptic damage, and improves learning and memory abilities in Alzheimer's disease mice. 8-F-2-(Me-Pip-Me)-Tryptanthrin can be used for the research of nervous system diseases, including diseases related to abnormal Tau protein phosphorylation and abnormal PSD-95 function .
Cat. No.: HY-183584
Target:
Research Areas:
ARN25699 is a kinase inhibitor with an IC50 of 5.5 nM against GSK-3β, 2.2 nM against FYN-α, and 242.3 nM against DYRK1A, and it exhibits oral bioavailability. ARN25699 reduces hyperphosphorylation of tau protein and promotes microtubule bundle formation. ARN25699 has a broader kinome inhibitory profile and targets kinases associated with the pathogenic mechanisms linked to Alzheimer's disease. ARN25699 can be used in the research of Alzheimer's disease and related tauopathies .
Cat. No.: HY-182028
Research Areas:
17β-HSD10-IN-4 is a selective brain-penetrant 17β-HSD10 inhibitor with an IC50 of 6.33 μM. 17β-HSD10-IN-4 forms key interactions with the 17β-HSD10 catalytic triad to functionally inhibit the enzyme, without altering its protein levels. 17β-HSD10-IN-4 restores mitochondrial function, reduces ROS levels, increases ATP production, and suppresses cytochrome c release. 17β-HSD10-IN-4 attenuates CDK5/p25 activation, reduces Tau hyperphosphorylation, Aβ plaque load and restores brain-derived neurotrophic factor levels. 17β-HSD10-IN-4 improves cognitive function.17β-HSD10-IN-4 can be used for the research of Alzheimer's disease .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
