GSK-3β/HDAC-IN-2
GSK-3β/HDAC-IN-2 is a potent inhibitor of GSK-3β (IC50 = 0.04 μM), HDAC2 (IC50 = 1.05 μM, Ki = 0.070 μM) and HDAC6 (IC50 = 1.52 μM, Ki = 0.017 μM). GSK-3β/HDAC-IN-2 inhibits HDAC2 and HDAC6 activities and blocks tau hyperphosphorylation. GSK-3β/HDAC-IN-2 exerts neuroprotective effects and shows no significant toxicity. GSK-3β/HDAC-IN-2 can be used in the research of Alzheimer's disease.
For research use only. We do not sell to patients.
- Formula: C12H11N5O5S
- Molecular Weight:337.31
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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GSK-3β 0.04 μM (IC50) |
HDAC6 1.52 μM (IC50) |
HDAC2 1.05 μM (IC50) |
HDAC6 0.017 μM (Ki) |
HDAC1 0.036 μM (Ki) |
HDAC3 0.066 μM (Ki) |
HDAC2 0.070 μM (Ki) |
HDAC8 0.772 μM (Ki) |
GSK-3β/HDAC-IN-2 (Compound 19) shows excellent level of inhibition at 15 μM against GSK-3β (100%), HDAC2 (86.51%), and HDAC6 (88.60%)[1].
GSK-3β/HDAC-IN-2 (0.1-100 μM, 24 h) shows no significant cytotoxicity and induced cell proliferation at a lower concentration (0.1 μM)[1].
GSK-3β/HDAC-IN-2 (10 μM, 17 h) completely counteractes copper mediated tau phosphorylation in differentiated SH-SY5Y cells induced by CuSO4 (400 μM, 16 h)[1].
GSK-3β/HDAC-IN-2 (0.5 μM, 24 h) reduces the CuSO4 (600 μM) neurotoxicity in SH-SY5Y cells[1].
GSK-3β/HDAC-IN-2 (0.1-10 μM, 24 h) induces the leves of phospho-GSK-3β (Ser9) and acetylation levels of both histone H3 and tubulin[1].
GSK-3β/HDAC-IN-2 selectively induces apoptosis in response to mitotic stress, through chromatin remodeling,
histone modulation, and checkpoint disruption in SH-SY5Y cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SH-SY5Y cells
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Concentration:0.1, 1, 10, 25, 50, and 100 μM
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Incubation Time:24 h
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Result:Showed no significant cytotoxicity at 100 μM and induced cell proliferation at a lower concentration (0.1 μM).
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Cell Line:SH-SY5Y cells incubated with CuSO4 (600 μM) for 24 h
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Concentration:0.5 μM
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Incubation Time:24 h, co-incubated with CuSO4 (600 μM)
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Result:Displayed a significant ability to reduce the CuSO4 neurotoxicity with a neuroprotective activity of 96.1%.
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Cell Line:SH-SY5Y cells
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Concentration:0.1, 1, and 10 μM
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Incubation Time:24 h
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Result:Induced a dose-dependent increase in phospho-GSK-3β (Ser9) levels.
Induced a massive dose-dependent increase in the acetylation levels of both histone H3 and tubulin, starting from the concentration of 1 μM.
Chemical Information
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Molecular Weight 337.31
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Formula C12H11N5O5S
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SMILES
O=C(NO)C1=CC=C(CNC(NC2=NC=C([N+]([O-])=O)S2)=O)C=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
GSK-3β/HDAC-IN-2 Related Classifications
HY-174398 Related Classifications
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