GSK-3 inhibitor 4

SKU: orb2900517

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.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 2227279-83-4
• MW: 403.38
• Purity: >98% (HPLC)
• Formula: C₂₂H₁₅F₂N₅O
• SMILES: N(C(=O)C1=NC(NC2=CC=C(F)C=C2)=NC=C1)C=3C(=CC=NC3)C4=CC=C(F)C=C4
• Target: GSK-3

Bioactivity

• In Vivo:
  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. 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). 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).
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

GSK-3