GSK-3 inhibitor 3

SKU: orb1819108

Description

GSK-3 inhibitor 3 is a potent, selective, and brain-penetrant small molecule that inhibits GSK-3α/β with sub-nanomolar IC50 values. It demonstrates in vivo efficacy by reducing tau phosphorylation at S396 (IC50=10 nM) in an Alzheimer's disease mouse model, supporting its use in researching tauopathies and other neurological disorders.

Research Area

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

Key Properties

• CAS Number: 2227279-84-5
• MW: 410.4
• Purity: 99.89% (May vary between batches)
• Formula: C₂₃H₁₅FN₆O
• SMILES: N(C(=O)C1=NC(NC2=CC=C(C#N)C=C2)=NC=C1)C=3C(=CC=NC3)C4=CC=C(F)C=C4
• Target: Microtubule Associated,GSK-3
• Solubility: DMSO:5.63 mg/mL (13.72 mM)

Bioactivity

• Target IC50:
  GSK-3β:0.25 nM|CDK5:1.3 μM|CDK2:0.22 μM|GSK-3α:0.35 nM
• In Vivo:
  GSK-3 inhibitor 3 (Compound 34) (2 mg/kg; i.v.;10 mg/kg orally; Alzheimer’s disease model using LaFerla 3xTg-C57BL6 mice) demonstrated a T1/2 of 2.5 hours (i.v.) in male C57BL6 mice and an oral bioavailability (F%) of approx. 100%. GSK-3 inhibitor 3 (10 mg/kg, single oral dose) reduces Tau 396 phosphorylation levels by 33% in a triple transgenic mouse model of Alzheimer's disease.
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• In Vitro:
  GSK-3 inhibitor 3 (Compound 34) (1 μM) is a highly selective inhibitor of CDK2 and CDK5 with IC50s of 0.22 μM and 1.3 μM for CDK2 and CDK5, respectively.
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Storage & Handling

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

Alternative Names

Microtubule Associated, MicrotubuleAssociated, GSK3, GSK-3, GSK-3 inhibitor 3, GSK3inhibitor3, tau

Compound Identifiers

PubChem CID

134556469