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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.

Sinônimo(s):

IKK Inhibitor VII, IKK 16

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About This Item

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

Nível de qualidade

Ensaio

≥97% (HPLC)

forma

solid

fabricante/nome comercial

Calbiochem®

condição de armazenamento

OK to freeze
protect from light

cor

pale yellow

solubilidade

DMSO: 10 mg/mL

Condições de expedição

wet ice

temperatura de armazenamento

−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)

chave InChI

BWZJBXAPRCVCKQ-UHFFFAOYSA-N

Descrição geral

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).

Ações bioquímicas/fisiológicas

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

Embalagem

Packaged under inert gas

Advertência

Toxicity: Harmful (C)

Informações legais

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

Código de classe de armazenamento

11 - Combustible Solids

Classe de risco de água (WGK)

WGK 3

Ponto de fulgor (°F)

Not applicable

Ponto de fulgor (°C)

Not applicable


Certificados de análise (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
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
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)
A frequent SNP in TRIM5I? strongly enhances the innate immune response against LINE-1 elements.
Lagisquet, et al.
Frontiers in Immunology, 14, 1168589-1168589 (2023)

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