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Merck

481407

NF-κB Activation Inhibitor

InSolution, ≥98%

別名:

InSolution NF-κB Activation Inhibitor

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この商品について

実験式(ヒル表記法):
C22H20N4O
分子量:
356.42
NACRES:
NA.77
UNSPSC Code:
12352200
Assay:
≥98% (HPLC)
Form:
liquid
Quality level:
Storage condition:
OK to freeze, desiccated (hygroscopic), protect from light
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Quality Level

assay

≥98% (HPLC)

form

liquid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, desiccated (hygroscopic), protect from light

shipped in

wet ice

storage temp.

2-8°C

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
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)


保管分類

10 - Combustible liquids

wgk

WGK 2

flash_point_f

188.6 °F - closed cup - (Dimethylsulfoxide)

flash_point_c

87 °C - closed cup - (Dimethylsulfoxide)


適用法令

試験研究用途を考慮した関連法令を主に挙げております。化学物質以外については、一部の情報のみ提供しています。 製品を安全かつ合法的に使用することは、使用者の義務です。最新情報により修正される場合があります。WEBの反映には時間を要することがあるため、適宜SDSをご参照ください。

Group 4: Flammable liquids + Type 3 petroleums + Hazardous rank III + Water insoluble liquid

fsl

481407-1MG:

jan



試験成績書(COA)

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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)



グローバルトレードアイテム番号

カタログ番号GTIN
481407-1MGCN04055977201512