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401486

Sigma-Aldrich

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.

Sinónimos:

IKK Inhibitor VII, IKK 16

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About This Item

Fórmula empírica (notación de Hill):
C28H29N5OS
Número de CAS:
Peso molecular:
483.63
UNSPSC Code:
12352200
NACRES:
NA.28

Quality Level

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

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

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.
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. 505378).

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

Packaging

Packaged under inert gas

Warning

Toxicity: Harmful (C)

Legal Information

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

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


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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
Sabine Matou-Nasri et al.
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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
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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
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Ocular exposure to particulate matter (PM) causes local inflammation; however, the influence of neutrophils on PM-induced ocular inflammation is still not fully understood. In this study, we constructed a system to investigate the role of PM in ocular inflammation using

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