Biochem/physiol Actions

Reversible: yes

Cell permeable: yes

Primary TargetKDM4

General description

A cell-permeable, non-toxic, n-octyl ester form of 5-carboxy-8-hydroxyquinoline (IOX1, Cat. No. 420201) that acts as a superior inhibitor of Jumonji C domain histone lysine demethylase. Shown to be about 30 fold more potent than IOX1 (EC₅₀ = 3.8 µM for KDM4A in HeLa cells vs. 100 µM for IOX1). Inhibits the H3K9 me3 demethylation activity of KDM4C (IC₅₀ = 3.9 µM in ALPHA Screen assay). Exhibits greater stability to hydrolysis in the ALPHA Screen buffer.

A cell-permeable, non-toxic, n-octyl ester form of 5-carboxy-8-hydroxyquinoline (IOX1, Cat. No. 420201) that acts as a superior inhibitor of Jumonji C domain histone lysine demethylase. Shown to be about 30 fold more potent than IOX1 (EC₅₀ = 3.8 µM for KDM4A in HeLa cells vs. 100 µM for IOX1). Inhibits the H3K9 me3 demethylation activity of KDM4C (IC₅₀ = 3.9 µM in ALPHA Screen assay). Exhibits greater stability to hydrolysis in the ALPHA Screen buffer.Please note that the molecular weight for this compound is batch-specific due to variable water content.

Legal Information

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

Other Notes

Schiller, R., et al. 2014. ChemMedChem.9,566.

Packaging

Packaged under inert gas

10 mg in Glass bottle

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Standard Handling (A)