GSK-3β inhibitor 2

SKU: orb1309607

Description

GSK-3β inhibitor 2

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1702428-31-6
• MW: 318.35
• Purity: 99.08% (May vary between batches)
• Formula: C₁₄H₁₄N₄O₃S
• SMILES: COc1nc(sc1C(N)=O)-c1ccnc(NC(=O)C2CC2)c1
• Target: GSK-3
• Solubility: DMSO:5 mg/mL (15.71 mM)

Bioactivity

• Target IC50:
  GSK-3β:1.1 nM
• In Vivo:
  In LaFerla 3xTg-C57BL6 mice with Alzheimer’s disease, GSK-3β inhibitor 2 (30 mg/kg; oral) significantly reduces hyperphosphorylated Tau396. GSK-3β inhibitor 2 shows only modest brain exposure (B/P = 0.26), determined as a single time point.
• In Vitro:
  The pyridine carboxamide of GSK-3β inhibitor 2 forms hydrogen bonds with the hinge V135 backbone amide, while the carbonyl oxygen of the thiazolyl primary amide establishes a critical hydrogen bond with K85. Single crystal X-ray diffraction confirms intramolecular hydrogen bonding between the methoxy -O- and the amide N-H in GSK-3β inhibitor 2 .

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

5-Thiazolecarboxamide,2-[2-[(cyclopropylcarbonyl)amino]-4-pyridinyl]-4-methoxy-, GSK3, GSK-3β inhibitor 2, GSK-3β, GSK-3b inhibitor 2, GSK-3beta inhibitor 2

Compound Identifiers

PubChem CID

73333976