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[1].

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

GSK-3β/HDAC-IN-2 Chemical Structure

GSK-3β/HDAC-IN-2 Chemical Structure

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GSK-3β/HDAC-IN-2 Related Antibodies

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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]

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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