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Merck

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.

Synonyme(s) :

IKK Inhibitor VII, IKK 16

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About This Item

Formule empirique (notation de Hill) :
C28H29N5OS
Numéro CAS:
873225-46-8
Poids moléculaire :
483.63
MDL number:
MFCD23704180
UNSPSC Code:
12352200
NACRES:
NA.28

Nom du produit

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.

Quality Level

100

SMILES string

[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

assay

≥97% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

pale yellow

solubility

DMSO: 10 mg/mL

shipped in

wet ice

storage temp.

−20°C

Catégories apparentées

Biochem/physiol Actions

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

Disclaimer

Toxicity: Harmful (C)

General description

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).

Packaging

Packaged under inert gas

Legal Information

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

Classe de stockage

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificats d'analyse (COA)

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Consulter la Bibliothèque de documents

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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Contenu apparenté

Pathways and Biomarkers of Toll-like Receptor (TLR) Signaling

"Toll-like Receptors (TLRs) are transmembrane proteins that are expressed on various immune cells. The extracellular N-terminal region of TLRs recognizes specific pathogen components. At least 13 different members of TLR family have been identified that detect different pathogen associated molecular patterns (PAMPs), including lipopolysaccharides, flagellin, bacterial CpG DNA, and viral RNA and DNA. Recognition of PAMPs by TLRs is considered as a key process for the induction of an inflammatory response."

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