Tyrphostin AG 538

SKU: orb1741449

Description

Tyrphostin AG 538 is a cell-permeable, reversible, and competitive chalcone inhibitor of the IGF-1 receptor kinase with an IC₅₀ of 400 nM. It is used in research to study IGF-1R signaling in cancer biology and has been applied in both in vitro and in vivo experimental models.

Research Area

Signal Transduction

Key Properties

• CAS Number: 133550-18-2
• MW: 297.26
• Purity: 98.75% (May vary between batches)
• Formula: C₁₆H₁₁NO₅
• SMILES: C(/C(=C/C1=CC(O)=C(O)C=C1)/C#N)(=O)C2=CC(O)=C(O)C=C2
• Target: IGF-1R
• Solubility: DMSO:4.5 mg/mL (15.14 mM)

Bioactivity

• Target IC50:
  IGF-1:400 nM|NS3-DNA complex:3.6 μM
• In Vivo:
  Typical assays used to discover and analyze small molecules that inhibit the hepatitis C virus (HCV) NS3 helicase yield few hits and are often confounded by compound interference. FP-based assay was chosen to screen Sigma's Library of Pharmacologically Active Compounds (LOPAC) for compounds that inhibit NS3-DNA complex formation. Four LOPAC compounds inhibited the FP-based assay: aurintricarboxylic acid (ATA) (IC50=1.4 μM), suramin sodium salt (IC50=3.6 μM), NF 023 hydrate (IC50=6.2 μM) and tyrphostin AG 538 (IC50=3.6 μM).
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• In Vitro:
  Experimentally it is indeed found that AG 538 does not compete with ATP but competes with the IGF-1R substrate. Both AG 538 and I-OMe AG 538 inhibit IGR-1R autophosphorylation in intact cells in a dose-dependent manner. Both compounds inhibit the activation of the downstream targets PKB and Erk2.
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Storage & Handling

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

Alternative Names

AG 538, AG538, AG-538, IGF1R, IGF-1R, Tyrphostin AG538, Tyrphostin AG-538, Tyrphostin AG 538

Compound Identifiers

PubChem CID

5328760