481406

NF-κB Activation Inhibitor

The NF-κB Activation Inhibitor, also referenced under CAS 545380-34-5, controls the biological activity of NF-κB. This small molecule/inhibitor is primarily used for Inflammation/Immunology applications.

• Synonym(s): NF-κB Activation Inhibitor, 6-Amino-4-(4-phenoxyphenylethylamino)quinazoline
• Empirical Formula (Hill Notation): C₂₂H₂₀N₄O
• CAS Number: 545380-34-5
• Molecular Weight: 356.42
• MDL number: MFCD06411436
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• Assay: ≥98% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: off-white
• solubility: DMSO: 5 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C
• InChI: 1S/C22H20N4O/c23-17-8-11-21-20(14-17)22(26-15-25-21)24-13-12-16-6-9-19(10-7-16)27-18-4-2-1-3-5-18/h1-11,14-15H,12-13,23H2,(H,24,25,26)
• InChI key: IBAKVEUZKHOWNG-UHFFFAOYSA-N

Description

General description

A cell-permeable quinazoline compound that acts as a highly potent inhibitor of NF-κB transcriptional activation (IC₅₀ = 11 nM in Jurkat cells) and LPS-induced TNF-α production (IC₅₀ = 7 nM in murine splenocytes). Shown to exhibit anti-inflammatory effect on carrageenin-induced paw edema in rat. A 10 mM (1 mg/281 µl) solution of NF-κB Activation Inhibitor (Cat. No. 481407) in DMSO is also available.

A cell-permeable quinazoline compound that acts as a potent inhibitor of NF-κB transcriptional activation (IC₅₀ = 11 nM in Jurkat cells) and LPS-induced TNF-α production (IC₅₀ = 7 nM in murine splenocytes). Does not exhibit cellular cytotoxicity even at concentrations as high as 10 µM. Reported to exhibit anti-inflammatory effects on carregeenin-induced paw edema in rats.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
NF-κB transcriptional activation

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 11 nM against NF-κB transcriptional activation in Jurkat cells

Packaging

Packaged under inert gas

Warning

Toxicity: Toxic (F)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Due to the nature of the Hazardous Materials in this shipment, additional shipping charges may be applied to your order. Certain sizes may be exempt from the additional hazardous materials shipping charges. Please contact your local sales office for more information regarding these charges.

Tobe, M., et al. 2003. Bioorg. Med. Chem.11, 383.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3