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Merck
CN

401486

IKK Inhibitor VII

The IKK Inhibitor VII, also referenced under CAS 873225-46-8, controls the biological activity of IKK. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

别名:

IKK Inhibitor VII, IKK 16

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关于此项目

经验公式(希尔记法):
C28H29N5OS
化学文摘社编号:
分子量:
483.63
MDL编号:
UNSPSC代码:
12352200
NACRES:
NA.28
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质量水平

方案

≥97% (HPLC)

表单

solid

制造商/商品名称

Calbiochem®

储存条件

OK to freeze
protect from light

颜色

pale yellow

溶解性

DMSO: 10 mg/mL

运输

wet ice

储存温度

−20°C

SMILES字符串

[s]1c2c(cc1c3nc(ncc3)Nc4ccc(cc4)C(=O)N5CCC(CC5)N6CCCC6)cccc2

InChI

1S/C28H29N5OS/c34-27(33-17-12-23(13-18-33)32-15-3-4-16-32)20-7-9-22(10-8-20)30-28-29-14-11-24(31-28)26-19-21-5-1-2-6-25(21)35-26/h1-2,5-11,14,19,23H,3-4,12-13,15-18H2,(H,29,30,31)

InChI key

BWZJBXAPRCVCKQ-UHFFFAOYSA-N

一般描述

A cell-permeable benzamido-pyrimidine compound that acts as a potent, selective, and ATP-competitive inhibitor of IKK (IC50 = 40 nM, 70 nM, and 200 nM for IKK-2, IKK complex, and IKK-1, respectively). Inhibits cellular IκBα degradation and NF-κB-mediated gene expression in vitro in HUVEC cells and has been shown to exhibit excellent in vivo efficacy both in mice and rats. Also available as a 10 mM solution in DMSO (Cat. No. 5.05378).

生化/生理作用

Cell permeable: yes
Primary Target
IKK
Product competes with ATP.
Reversible: no
Target IC50: 40 nM, 70 nM, and 200 nM for IKK-2, IKK complex, and IKK-1, respectively

包装

Packaged under inert gas

法律信息

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

免责声明

Toxicity: Harmful (C)

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable


分析证书(COA)

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Rudolf Waelchli et al.
Bioorganic & medicinal chemistry letters, 16(1), 108-112 (2005-10-21)
The design, synthesis, and the biological evaluation of 2-benzamido-pyrimidines as novel IKK inhibitors are described. By optimization of the lead compound 3, compounds 16 and 24 are identified as good inhibitors of IKK2 with IC(50) values of 40 and 25
Y Liu et al.
Journal of immunology research, 2023, 1884439-1884439 (2023-01-28)
Platelets have toll-like receptors (TLRs); however, their function in thrombosis or hemostasis under flow conditions is not fully known. Thrombin-inhibited anticoagulated whole blood was treated with various TLR agonists and then perfused over fibrillar collagen using microfluidic assay at venous
ATP Consumption Is Coupled with Endocytosis in Exudated Neutrophils.
Wang, et al.
International Journal of Molecular Sciences, 24 (2023)
Sabine Matou-Nasri et al.
PloS one, 17(5), e0267855-e0267855 (2022-05-06)
Most of the AML patients in remission develop multidrug resistance after the first-line therapy and relapse. AML stem cells have gained attention for their chemoresistance potentials. Chemoresistance is a multifactorial process resulting from altered survival signaling pathways and apoptosis regulators
Mai Tuyet Nguyen et al.
PloS one, 17(8), e0269735-e0269735 (2022-08-03)
We previously showed that the matricellular protein CCN5 reverses established cardiac fibrosis (CF) through inducing apoptosis in myofibroblasts (MyoFBs) but not in cardiomyocytes or fibroblasts (FBs). In this study, we set out to elucidate the molecular mechanisms underlying CCN5-mediated selective

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