assay
≥98% (HPLC)
form
liquid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, desiccated (hygroscopic), protect from light
shipped in
wet ice
Quality Level
General description
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
NF-κB transcriptional activation
Product does not compete with ATP.
Reversible: no
Target IC50: 11 nM against NF-κB transcriptional activation in Jurkat cells; 7 nM against LPS-induced TNF-α production in murine splenocytes
Packaging
Packaged under inert gas
Physical form
A 10 mM (1 mg/281 µl) solution of NF-κB Activation Inhibitor (Cat. No. 481406) in DMSO.
Preparation Note
Following initial use, aliquot and refrigerate (4°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
Disclaimer
Toxicity: Toxic (F)
存储类别
10 - Combustible liquids
wgk
WGK 2
flash_point_f
188.6 °F - closed cup - (Dimethylsulfoxide)
flash_point_c
87 °C - closed cup - (Dimethylsulfoxide)
Discovery of quinazolines as a novel structural class of potent inhibitors of NF-kappa B activation.
Masanori Tobe et al.
Bioorganic & medicinal chemistry, 11(3), 383-391 (2003-01-09)
We disclose here a new structural class of low-molecular-weight inhibitors of NF-kappa B activation that were designed and synthesized by starting from quinazoline derivative 6a. Structure-activity relationship (SAR) studies based on 6a elucidated the structural requirements essential for the inhibitory
Differential regulation of transcription factor T-bet induction during NK cell development and T helper-1 cell differentiation.
Fang, et al.
Immunity, 55, 639-655 (2023)
Eunbi Ko et al.
Experimental dermatology, 24(12), 936-941 (2015-07-16)
House dust mites (HDMs) are known to trigger chronic inflammation through Toll-like receptors (TLRs) and their signalling cascades. In this study, we found that TLR2 ligation by HDMs induced the activation of dual oxidase 2 (Duox2) and nuclear factor-κB (NF-κB)
Fatmah A Mansour et al.
Oncoimmunology, 9(1), 1729299-1729299 (2020-04-22)
The T-cell inhibitory molecule PD-L1 is expressed on a fraction of breast cancer cells. The distribution of PD-L1 on the different subpopulations of breast cancer cells is not well-defined. Our aim was to study the expression level of PD-L1 on
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