2. PI3K/Akt/mTOR Stem Cell/Wnt Cell Cycle/DNA Damage Epigenetics Neuronal Signaling
  3. GSK-3 HDAC Tau Protein
  4. 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.

GSK-3β/HDAC-IN-2

GSK-3β/HDAC-IN-2 Chemical Structure

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GSK-3β/HDAC-IN-2 Related Antibodies

Top Publications Citing Use of Products

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GSK-3 GSK-3α GSK-3β

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HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

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Description

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[1].

IC50 & Target[1]

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)

In Vitro

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, pretreated with 1 h and then co-incubated for 16 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.

GSK-3β/HDAC-IN-2 Related Antibodies

Cell Cytotoxicity Assay[1]

Cell Line: SH-SY5Y cells
Concentration: 0.1, 1, 10, 25, 50, and 100 μM
Incubation Time: 24 h
Result: Showed no significant cytotoxicity at 100 μM and induced cell proliferation at a lower concentration (0.1 μM).

Cell Cytotoxicity Assay[1]

Cell Line: SH-SY5Y cells incubated with CuSO4 (600 μM) for 24 h
Concentration: 0.5 μM
Incubation Time: 24 h, co-incubated with CuSO4 (600 μM)
Result: Displayed a significant ability to reduce the CuSO4 neurotoxicity with a neuroprotective activity of 96.1%.

Western Blot Analysis[1]

Cell Line: SH-SY5Y cells
Concentration: 0.1, 1, and 10 μM
Incubation Time: 24 h
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.
Molecular Weight

337.31

Formula

C12H11N5O5S
SMILES

O=C(NO)C1=CC=C(CNC(NC2=NC=C([N+]([O-])=O)S2)=O)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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GSK-3β/HDAC-IN-2 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    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.

Keywords:

GSK-3β/HDAC-IN-2GSK-3HDACTau ProteinGlycogen synthase kinase-3Glycogen synthase kinase 3Histone deacetylasesAlzheimer’s disease (AD)Glycogen Synthase Kinase 3β (GSK-3β)Histone Deacetylases (HDACs)HDAC2HDAC6SH-SY5Y cellsInhibitorinhibitorinhibit

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