2. PI3K/Akt/mTOR Stem Cell/Wnt Neuronal Signaling
  3. GSK-3 Tau Protein Amyloid-β β-catenin
  4. Multitarget AD-IN-7

Multitarget AD-IN-7 is an orally active multi-target anti-AD compound. Multitarget AD-IN-7 exhibits inhibitory activity against GSK-3β and GSK-3α (IC50 = 0.66, 0.83 nM). Multitarget AD-IN-7 upregulates the expression of p-GSK-3β-Ser9, inhibits the phosphorylation of tau-Ser396, targets Aβ1-42, chelates pathogenic metal ions, scavenges ABTS•+, upregulates the expression of β-catenin and neurogenesis biomarkers, and promotes neurite outgrowth. Multitarget AD-IN-7 improves motor ability in Alzheimer's disease zebrafish. Multitarget AD-IN-7 is applicable to research related to Alzheimer's disease.

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Multitarget AD-IN-7

Multitarget AD-IN-7 Chemical Structure

CAS No. : 3113741-59-3

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Multitarget AD-IN-7 Related Antibodies

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Description

Multitarget AD-IN-7 is an orally active multi-target anti-AD compound. Multitarget AD-IN-7 exhibits inhibitory activity against GSK-3β and GSK-3α (IC50 = 0.66, 0.83 nM). Multitarget AD-IN-7 upregulates the expression of p-GSK-3β-Ser9, inhibits the phosphorylation of tau-Ser396, targets Aβ1-42, chelates pathogenic metal ions, scavenges ABTS•+, upregulates the expression of β-catenin and neurogenesis biomarkers, and promotes neurite outgrowth. Multitarget AD-IN-7 improves motor ability in Alzheimer's disease zebrafish. Multitarget AD-IN-7 is applicable to research related to Alzheimer's disease[1].

IC50 & Target[1]

GSK-3β

0.66 nM (IC50)

GSK-3α

0.83 nM (IC50)

In Vitro

Multitarget AD-IN-7 (Compound 3c) exhibits excellent selectivity for GSK-3β/α in a screening panel consisting of 24 kinases, with an IC50 of 0.83 nM against GSK-3α and an IC50 of 928 nM against CDK5/p35[1].
Multitarget AD-IN-7 (1-10 μM; 2.5 h) upregulates the level of p-GSK-3β-Ser9, thereby inactivating GSK-3β in SH-SY5Y cells, and upregulates the level of β-catenin in SH-SY5Y cells[1].
Multitarget AD-IN-7 (1-10 μM; 1 h pre-incubation prior to 6 h Aβ25-35 stimulation) inhibits Aβ25-35 (HY-P0128)-induced tau-Ser396 phosphorylation in SH-SY5Y cells in a concentration-dependent manner in vitro[1].
Multitarget AD-IN-7 (10 μM; 24 h) upregulates the mRNA expression levels of neurogenesis-related biomarkers GAP-43 and MAP-2 in SH-SY5Y cells[1].
Multitarget AD-IN-7 (1 μM; 72 h) promotes axonal growth in SH-SY5Y cells, increasing the proportion of cells with axons to 44.11%[1].
Multitarget AD-IN-7 (20 μM mixed with 40 μM metal ions; 30 min at ambient temperature) exhibits strong chelation with Alzheimer's disease (AD)-related metal ions Fe2+, Zn2+, Cu2+ and Al3+ (but does not chelate Na+, K+, Mg2+ or Ca2+)[1].
Multitarget AD-IN-7 (20 μM mixed with 20 μM Aβ1-42; 24 h at 37 °C) inhibits the self-aggregation of Aβ1-42 with an inhibition rate of 33.35% and disaggregates preformed Aβ1-42 aggregates by 46.48%, as detected by ThT fluorescence assay and transmission electron microscopy (TEM)[1].
Multitarget AD-IN-7 (20 μM mixed with 20 μM Aβ1-42 and 20 μM Cu2+; 24 h at 37 °C) exhibits 52.18% inhibition of Cu2+-mediated Aβ1-42 aggregation and achieves a 56.12% disaggregation rate of preformed Cu2+-Aβ1-42 aggregates, as determined by ThT fluorescence assay[1].
Multitarget AD-IN-7 exhibits an IC50 of 7.04 μM for scavenging ABTS•+[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Multitarget AD-IN-7 Related Antibodies

Western Blot Analysis[1]

Cell Line: SH-SY5Y cells
Concentration: 1, 5, 10 μM
Incubation Time: 2.5 h
Result: Increased p-GSK-3β-Ser9 levels in a concentration-dependent manner, with p-GSK-3β-Ser9/GAPDH ratios of 0.43, 0.63, and 0.76 for 1, 5, 10 μM, respectively.\nIncreased β-catenin levels in a concentration-dependent manner, with β-catenin/GAPDH ratios of 0.32, 0.39, and 0.51 for 1, 5, 10 μM, respectively.

Western Blot Analysis[1]

Cell Line: SH-SY5Y cells
Concentration: 1, 5, 10 μM
Incubation Time: 1 h (pre-incubation before 6 h Aβ25-35 stimulation)
Result: Decreased p-tau-Ser396 levels in a concentration-dependent manner, with p-tau-Ser396/GAPDH ratios of 0.31, 0.24, and 0.18 for 1, 5, 10 μM, respectively.

RT-PCR[1]

Cell Line: SH-SY5Y cells
Concentration: 10 μM
Incubation Time: 24 h
Result: Upregulated mRNA expression of GAP-43 and MAP-2 to levels greater than the positive control retinoic acid.
In Vivo

Multitarget AD-IN-7 (1.95-7.81 μM; water exposure; 24 h) dose-dependently enhances the motor ability of AlCl3-induced Alzheimer's disease zebrafish[1].
Multitarget AD-IN-7 (1000 mg/kg; p.o.; single dose) exhibits low acute toxicity in C57BL/6 mice. No mortality, behavioral abnormalities, body weight changes or organ pathological alterations are observed within 14 days after a single oral dose of 1000 mg/kg[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: AB wild-type (juvenile, 4 days post-fertilization)[1]
Dosage: 1.95 μM; 3.91 μM; 7.81 μM
Administration: water exposure; 24 h
Result: Increased swimming distance of AlCl3-induced AD zebrafish to 1314 mm at 1.95 μM.
Increased swimming distance of AlCl3-induced AD zebrafish to 1716 mm at 3.91 μM.
Increased swimming distance of AlCl3-induced AD zebrafish to 2040 mm at 7.81 μM, compared to the AlCl3-induced control distance of 996 mm.
Animal Model: C57BL/6 (6-8 weeks old, male and female)[1]
Dosage: 1000 mg/kg
Administration: p.o.; single dose
Result: Observed no mortalities or abnormal behaviors over 14 days.
Showed no marked body weight changes compared to controls.
Observed no noticeable size or shape differences in dissected organs (heart, liver, spleen, lung, kidney, brain).
Revealed no significant pathological changes in organs via H&E staining.
Molecular Weight

457.48

Formula

C28H19N5O2
CAS No.
SMILES

OC1=CC(C2=CN=C(NC=C3C(NC4=C(C5=CC=CC=C5)C=CN=C4)=O)C3=C2)=CC6=C1N=CC=C6
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Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Multitarget AD-IN-7 Related Classifications

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Keywords:

Multitarget AD-IN-73113741-59-3GSK-3Tau ProteinAmyloid-ββ-cateninGlycogen synthase kinase-3Glycogen synthase kinase 3β-amyloid peptideAβAbetaBeta cateninMulti-target AD inhibitorsAlzheimer's diseaseSH-SY5Y cellsZebrafishC57BL/6 miceInhibitorinhibitorinhibit

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