5.05378

IKK Inhibitor VII

InSolution, ≥97%, 10 mM in DMSO, potent, selective, and ATP-competitive inhibitor of IKK

• Synonym(s): InSolution IKK Inhibitor VII, (4-(4-(Benzo[b]thiophen-2-yl)pyrimidin-2-ylamino)phenyl)(4-(pyrrolidin-1-yl)piperidin-1-yl)methanone, InSolution IKK Inhibitor VII, IKK 16, IKK 16, (4-(4-(Benzo[b]thiophen-2-yl)pyrimidin-2-ylamino)phenyl)(4-(pyrrolidin-1-yl)piperidin-1-yl)methanone, InSolution IKK Inhibitor VII
• Empirical Formula (Hill Notation): C₂₈H₂₉N₅OS
• CAS Number: 873225-46-8
• Molecular Weight: 483.63
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• assay: ≥97% (HPLC)
• form: liquid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; avoid repeated freeze/thaw cycles; desiccated (hygroscopic); protect from light
• storage temp.: −70°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

Description

General description

A cell-permeable benzamido-pyrimidine compound that acts as a potent, selective, and ATP-competitive inhibitor of IKK (IC₅₀ = 40, 70, 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.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
IKK-2, IKK complex, and IKK-1

Reversible: yes

Packaging

Packaged under inert gas

Warning

Toxicity: Irritant (B)

Physical form

A 10 mM (500 µg/103 µL) sterile-filtered solution of IKK Inhibitor VII (Cat. No. 401486) in DMSO.

Reconstitution

Following initial thaw, aliquot and freeze (-20°C). Aliquots are stable for up to 6 months at -20°C.

Other Notes

Waelchli, R., et al. 2006. Bioorg. Med. Chem. Lett.16, 108.

Legal Information

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