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481406

Sigma-Aldrich

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

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About This Item

Empirical Formula (Hill Notation):
C22H20N4O
CAS Number:
Molecular Weight:
356.42
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

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

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

Storage Class Code

11 - Combustible Solids

WGK

WGK 3


Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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