W2A-28
W2A-28 is a daul modulator of class I HDACs and Wnt/β-catenin. W2A-28 inhibits HDAC1, 2 and 3 activities with IC50 values of 512, 675, and 217 nM, respectively. W2A-28 shows selectivity over other HDACs and Sirtuin family members. W2A-28 activates Wnt/β-catenin signaling via reduced LRP6 degradation, enhances histone acetylation, suppresses tau phosphorylation, and reduces Aβ40 and Aβ42 levels. W2A-28 can be used for the research of Alzheimer's disease.
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- CAS No.: 2803203-72-5
- Formule: C14H14N4O2
- Masse moléculaire:270.29
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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- Pureté et documentation
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Activité biologique
Description
In Vitro
W2A-28 potently activates Wnt/β-catenin signaling in Wnt-3A-expressing HEK293 cells with an EC50 of 1.61 µM[1].
W2A-28 (8 µM; 24 h) significantly upregulates β-catenin protein levels in N2a neuroblastoma cells[1].
W2A-28 (2-4 µM; 24 h) significantly upregulates LRP6 protein levels in HA-tagged LRP6-expressing HT1080 cells[1].
W2A-28 (1-2 µM; 3 days) enhances histone acetylation, activates Wnt/β-catenin signaling, and significantly inhibits tau phosphorylation in cerebral organoids carrying APOE ε4/ε4 or APOE ε3/ε4 with PSEN1M146V mutation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HA-tagged LRP6-expressing HT1080 cells
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Concentration:2; 4 µM
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Incubation Time:24 h
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Result:Significantly increased LRP6 protein levels relative to vehicle control at 2 µM and 4 µM.
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Cell Line:Human cerebral
organoids carrying APOE ε4/ε4 or APOE ε3/ε4 with PSEN1M146V mutation -
Concentration:1; 2 µM
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Incubation Time:3 days
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Result:greatly increased the levels of histone H3 acetylation in iPSC-derived cerebral organoids, at 1 and 2 µM.
Significantly increased total cellular β-catenin levels in organoids.
Significantly increased NeuroD1 protein levels in organoids.
Inhibited tau phosphorylation.
Chemical Information
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CAS No. 2803203-72-5
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Masse moléculaire 270.29
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Formule C14H14N4O2
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SMILES
NC1=C(NC(C2=NC=C(NC(C)=O)C=C2)=O)C=CC=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
W2A-28 Related Classifications
HY-184177 Related Classifications
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