1. Cell Cycle/DNA Damage Epigenetics Stem Cell/Wnt Neuronal Signaling
  2. HDAC Wnt β-catenin Tau Protein Amyloid-β
  3. 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 40 and 42 levels. W2A-28 can be used for the research of Alzheimer's disease.

For research use only. We do not sell to patients.

W2A-28

W2A-28 Chemical Structure

CAS No. : 2803203-72-5

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Description

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 40 and 42 levels. W2A-28 can be used for the research of Alzheimer's disease[1][2].

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.

Western Blot Analysis[1]

Cell Line: HA-tagged LRP6-expressing HT1080 cells
Concentration: 2; 4 µM
Incubation Time: 24 h
Result: Significantly increased LRP6 protein levels relative to vehicle control at 2 µM and 4 µM.

Western Blot Analysis[1]

Cell Line: Human cerebral
organoids carrying APOE ε4/ε4 or APOE ε3/ε4 with PSEN1M146V mutation
Concentration: 1; 2 µM
Incubation Time: 3 days
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.
Molecular Weight

270.29

Formula

C14H14N4O2

CAS No.
SMILES

NC1=C(NC(C2=NC=C(NC(C)=O)C=C2)=O)C=CC=C1

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Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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W2A-28
Cat. No.:
HY-184177
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