2. PI3K/Akt/mTOR Stem Cell/Wnt Cell Cycle/DNA Damage
  3. GSK-3 CDK
  4. GSK-3 inhibitor 4

GSK-3 inhibitor 4 is an orally active and brain-penetrant inhibitor of GSK-3, CDK2, and CDK5, with IC50 values of 0.56 nM (GSK-3β), 0.45 nM (GSK-3α), 0.47 μM, and 0.68 μM, respectively. GSK-3 inhibitor 4 effectively reduces the phosphorylation level of Tau protein. GSK-3 inhibitor 4 can be used in Alzheimer's disease (AD) studies.

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GSK-3 inhibitor 4 Chemical Structure

GSK-3 inhibitor 4 Chemical Structure

CAS No. : 2227279-83-4

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GSK-3 inhibitor 4 Related Antibodies

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Description

GSK-3 inhibitor 4 is an orally active and brain-penetrant inhibitor of GSK-3, CDK2, and CDK5, with IC50 values of 0.56 nM (GSK-3β), 0.45 nM (GSK-3α), 0.47 μM, and 0.68 μM, respectively. GSK-3 inhibitor 4 effectively reduces the phosphorylation level of Tau protein. GSK-3 inhibitor 4 can be used in Alzheimer's disease (AD) studies[1].

IC50 & Target

GSK-3α

0.45 nM (IC50)

GSK-3β

0.56 nM (IC50)

CDK2

0.47 μM (IC50)

CDK5

0.68 μM (IC50)

In Vitro

GSK-3 inhibitor 4 (compound 40) exhibits excellent selectivity against CDK2 (840-fold, IC50 = 0.47 μM), CDK5 (1200-fold, IC50 = 0.68 μM), GSK-3β (IC50 = 0.56 nM), and GSK-3α (IC50 = 0.45 nM)[1].
GSK-3 inhibitor 4 has good permeability and exhibits a high ability to bind to plasma proteins and brain tissue due to its lipophilic nature[1].

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

GSK-3 inhibitor 4 Related Antibodies
In Vivo

GSK-3 inhibitor 4 (10 mg/kg, p.o.) produce a 37% reduction in pTau396, when administered orally as a nanosuspension at a dose of 10 mg/kg[1].
GSK-3 inhibitor 4 (2 mg/kg, i.v.; 10 mg/kg, p.o.) exhibite low-moderate clearance ranging from 15.8 to 23.3 mL/min/kg and are well-absorbed when administered orally as a solution[1].
Pharmacokinetic Parameters of GSK-3 Inhibitor 4 (compound 40) in Mice. [1]

小鼠体内 GSK-3 Inhibitor 4 (compound 40) 的药代动力学参数[1]

IV PK parameters oral PK parameters
CL (mL min-1 kg-1) Vdss (L/kg) MRT (h) t1/2 (h) AUCtot (μM•h) Cmax (μM) F%
18.9 2.6 2.3 2.8 11.7 1.5 53

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

Animal Model: 3xTg mice were bred onto the C57BL6 background and bred as homozygotes. Male animals between the ages of five to seven months were used for the study[1].
Dosage: 10 mg/kg
Administration: Oral gavage (p.o.)
Result: Produced a 37% reduction in pTau396, when administered orally as a nanosuspension at a dose of 10 mg/kg.
Animal Model: male C57BL6 mice (Pharmacokinetic assay)[1]
Dosage: 2 mg/kg, 10 mg/kg.
Administration: Kept for 8 h fasting prior to formulation administration. intravenous and oral routes of administration to mice at a dose of 2 and 10 mg/kg, respectively.
Result: Exhibited clearance ranging from 15.8 to 23.3 mL /min/kg , halflives ranging from 2.5 to 2.9 h and were readily orally bioavailable (F% = 53).
Molecular Weight

403.38

Formula

C22H15F2N5O
CAS No.
SMILES

O=C(C1=NC(NC2=CC=C(C=C2)F)=NC=C1)NC3=C(C4=CC=C(F)C=C4)C=CN=C3
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-3 inhibitor 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:

GSK-3 inhibitor 42227279-83-4GSK-3CDKGlycogen synthase kinase-3Glycogen synthase kinase 3Cyclin dependent kinaseGSK-3βGSK-3αCDK2CDK5GSK-3 inhibitorU2OSAlzheimer's diseaseADInhibitorinhibitorinhibit

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