2. PI3K/Akt/mTOR Stem Cell/Wnt Neuronal Signaling
  3. GSK-3 Tau Protein
  4. GSK3β-IN-4

GSK3β-IN-4 is a selective, potent, orally active and brain-penetrant ATP-competitive GSK3β inhibitor with an IC50 of 0.37 nM. GSK3β-IN-4 shows an IC50 of 2.75 nM and SI of 7.4 for GSK3α. GSK3β-IN-4 reduces tau phosphorylation at Ser396 by inhibiting GSK3β and imoroves cognitive deficits in Alzheimer's disease models. GSK3β-IN-4 can be used for the research of Alzheimer's disease.

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

GSK3β-IN-4

GSK3β-IN-4 Chemical Structure

CAS No. : 3083425-61-7

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GSK3β-IN-4 Related Antibodies

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Description

GSK3β-IN-4 is a selective, potent, orally active and brain-penetrant ATP-competitive GSK3β inhibitor with an IC50 of 0.37 nM. GSK3β-IN-4 shows an IC50 of 2.75 nM and SI of 7.4 for GSK3α. GSK3β-IN-4 reduces tau phosphorylation at Ser396 by inhibiting GSK3β and imoroves cognitive deficits in Alzheimer's disease models. GSK3β-IN-4 can be used for the research of Alzheimer's disease[1].

IC50 & Target[1]

GSK-3β

0.37 nM (IC50)

GSK-3α

2.75 nM (IC50)

In Vitro

GSK3β-IN-4 (Compound 39a) significantly inhibits Tau phosphorylation (EC50 = 0.06 μM) at Ser396 in Tau (P301L) 293T cells with low cytotoxicity (IC50= 80.75 μM)[1].
GSK3β-IN-4 inhibits GSK3β in an ATP-competitive manner with IC50 values of 1.27 nM, 7.14 nM, and 77.8 nM at 1 × Km, 10 × Km, and 100 × Km ATP concentrations, respectively[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

GSK3β-IN-4 Related Antibodies
Parmacokinetics
Species Dose Route T1/2 Cmax AUC0-t AUC0-∞ CL Vss Tmax F
Mice[1] 2.5 mg/kg i.v. 0.39 h 1.09 μg/mL 0.63 μg·h/mL 0.63 μg·h/mL 3.99 L/h/kg 2.24 L/kg 0.08 h /
Mice[1] 25 mg/kg p.o. 1.78 h 1.24 μg/mL 1.02 μg·h/mL 1.069 μg·h/mL / / 0.25 h 16.2 %
In Vivo

GSK3β-IN-4 (Compound 39a) (1000 mg/kg, p.o., single dose) shows no lethality in C57BL/6J mice, with normal body weight gain, no behavioral abnormalities within 14 days, and no pathological damage in major organs[1].
GSK3β-IN-4 (5-25 mg/kg, p.o., daily for 14 days) imoroves cognitive deficits and tau Ser396 phosphorylation levels in an Okadaic acid (HY-N6785)-induced mouse model of Alzheimer's disease[1].
GSK3β-IN-4 (5 mg/kg, p.o., once daily for 60 days) meliorates spatial learning and memory impairments in 6-month-old 3×Tg-AD mice, reduces Tau Ser396 phosphorylation in the hippocampal CA3 region, with efficacy comparable to Donepezil (HY-14566) (5 mg/kg), and shows no impact on motor function[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6J mice (Okadaic acid-induced model of Alzheimer's disease)[1]
Dosage: 5 mg/kg, 25 mg/kg
Administration: Orally administration
Result: Reduced tau phosphorylation (pS396) in the hippocampus and temporal.
Reduced escape latency and improved spatial memory retention, as evidenced by increased time spent in the target quadrant and higher platform-crossing frequency.
Did not cause locomotor dysfunction.
Animal Model: 3×Tg-AD mice (transgenic model of Alzheimer's disease)[1]
Dosage: 5 mg/kg
Administration: Orally administration
Result: Improved spatial learning and memory deficits.
Reduced escape latency during hidden platform trials and increased time spent in the target quadrant during probe tests.
Revealed a reduction in pS396 tau levels in the hippocampal CA3 region.
Molecular Weight

426.51

Formula

C26H26N4O2
CAS No.
SMILES

O=C(C1CCCC1)NC2=C3C(C4=CC=C(C(N[C@@H](C5=CC=CC=C5)C)=O)C=C4N3)=CC=N2
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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GSK3β-IN-4 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:

GSK3β-IN-43083425-61-7GSK-3Tau ProteinGlycogen synthase kinase-3Glycogen synthase kinase 3GSK3βTau phosphorylationSer396293TOkadaic acidTg-ADInhibitorinhibitorinhibit

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