NSC 228155

SKU: orb1300356

Description

NSC 228155 is a small molecule activator of the Epidermal Growth Factor Receptor (EGFR). It functions by binding to the dimerization domain (Domain II) of soluble EGFR, thereby modulating its tyrosine phosphorylation. This compound is utilized in biochemical and cellular research to study EGFR signaling pathways in both in vitro and in vivo experimental models.

Research Area

Cardiovascular Research, Cell Biology, Epigenetics & Chromatin, Molecular Biology, Signal Transduction

Key Properties

• CAS Number: 113104-25-9
• MW: 290.25
• Purity: 99.84%
• Formula: C₁₁H₆N₄O₄S
• SMILES: [O-][N+](=O)c1ccc(Sc2cccc[n+]2[O-])c2nonc12
• Target: Epigenetic Reader Domain,DNA/RNA Synthesis,Histone Acetyltransferase,EGFR
• Solubility: Ethanol:< 1 mg/mL (insoluble or slightly soluble);H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+90% Corn Oil:1 mg/mL (3.45 mM);DMSO:7.34 mg/mL (25.29 mM)

Bioactivity

• Target IC50:
  KIX-KID:0.36 μM
• In Vitro:
  NSC 228155 promotes transactivation of several RTKs, including ErbB2 and ErbB3, Insulin R and IGF-1 R receptors in the cells. It stimulates dimerization of sEGFR domain II. NSC 228155 can rapidly move across cell membranes and disperse within both cytoplasmic and nuclear compartments. It rapidly generates hydrogen peroxide within cells. NSC 228155 is also a potent inhibitor of KIX-KID interaction(IC50 = 0.36 μM), but it is not particularly selective against CREB-mediated gene transcription in HEK 293T cells.
• Cell Research:
  MDA MB468 cells serum-starved overnight are pre-incubated (or not) with 10 μM AG1478 or 2 μM PD 153035 for 90 min and then, where indicated, incubated with 100 μM NSC 228155 or CN 009543V or 150 ng/ml EGF or vehicle (0.2% DMSO) for 15 min. Proteins are blotted to nitrocellulose membrane and analyzed with biotinylated anti-pTyr P100, anti-pEGFR Y1068 and anti-EGFR (epitope in cytoplasmic region) antibodies. (Only for Reference)

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

DNA Synthesis, DNASynthesis, ErbB-1, Epigenetic Reader Domain, EpigeneticReaderDomain, Epidermal growth factor receptor, EGFR, Inhibitor, HER1, HistoneAcetyltransferase, Histone Acetyltransferase, HATs, HAT, inhibit, NSC 228155, NSC228155, NSC-228155, KIX-KID interaction, RNA Synthesis, RNASynthesis

Compound Identifiers

PubChem CID

313619