GSK-3 inhibitor 4

SKU: orb1905848

Description

GSK-3 inhibitor 4 is an orally bioavailable, brain-penetrant small molecule that potently inhibits GSK-3α/β and CDK2/5 kinases. It effectively reduces Tau protein levels in cellular models, making it a useful research tool for investigating Alzheimer's disease pathology and related tauopathies.

Research Area

Cell Biology, Pharmacology & Drug Discovery, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 2227279-83-4
• MW: 403.38
• Purity: 99.82% (May vary between batches)
• 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,CDK
• Solubility: DMSO:50 mg/mL (123.95 mM)

Bioactivity

• Target IC50:
  GSK-3β:0.56 nM|CDK5:0.68 μM|GSK-3α:0.45 nM|CDK2:0.47 μM
• In Vivo:
  GSK-3 inhibitor 4 (10 mg/kg; p.o.) reduced pTau396 by 37% when administered orally as a nanosuspension. GSK-3 inhibitor 4 (2 mg/kg, i.v.; 10 mg/kg, p.o.) exhibits low to moderate clearance (15.8 to 23.3 mL/min/kg) and is well absorbed orally in solution.
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• In Vitro:
  GSK-3 inhibitor 4 (compound 40) demonstrates excellent selectivity and efficacy 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). It also exhibits good permeability and a high capacity for binding to plasma proteins and brain tissue due to its lipophilicity.
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Storage & Handling

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

Alternative Names

CDK2, CDK5, GSK-3 inhibitor 4, GSK3inhibitor4, GSK3, GSK-3

Compound Identifiers

PubChem CID

134556675