401488

IKK-3 Inhibitor IX

The IKK-3 Inhibitor IX, also referenced under CAS 862812-98-4, controls the biological activity of IKK-3. This small molecule/inhibitor is primarily used for Inflammation/Immunology applications.

• Synonym(s): IKK-3 Inhibitor IX, 5-(5,6-Dimethoxybenzimidazol-1-yl)-3-(2-methanesulfonyl-benzyloxy)-thiophene-2-carbonitrile
• Empirical Formula (Hill Notation): C₂₂H₁₉N₃O₅S₂
• CAS Number: 862812-98-4
• Molecular Weight: 469.53
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• Assay: ≥95% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: beige
• solubility: DMSO: 10 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C
• InChI: 1S/C22H19N3O5S2/c1-28-17-8-15-16(9-18(17)29-2)25(13-24-15)22-10-19(20(11-23)31-22)30-12-14-6-4-5-7-21(14)32(3,26)27/h4-10,13H,12H2,1-3H3
• InChI key: LDTAHRLHGHFHKP-UHFFFAOYSA-N

Description

General description

A thiophenecarbonitrile compound that acts as a potent ATP-competitive inhibitor of IKK-3 (IKK-ε, IC₅₀ = 40 nM) with ~20-fold selectivity over PLK1 and more than 125-fold selectivity over a panel of 9 other commonly studied kinases, including IKK-1/2 (IKK-α/β). Reported to be inactive against cytochrome P450 isozymes (IC₅₀<50 µM) 1A2, 2D6, 2C9, and 3A4.

Biochem/physiol Actions

Cell permeable: no

Primary Target
IKK-3

Product competes with ATP.

Reversible: no

Target IC₅₀: 40 nM against IKK-3 (IKK-ε)

Packaging

Packaged under inert gas

Warning

Toxicity: Harmful (C)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Bamborough, P., et al. 2006. Bioorg. Med. Chem. Lett.16, 6236.

Legal Information

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 2
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable