5.30537

JmjC Histone Demethylase Inhibitor, n-Octyl-IOX1

• Synonym(s): JmjC Histone Demethylase Inhibitor, n-Octyl-IOX1, KDM4 Inhibitor
• Empirical Formula (Hill Notation): C₁₈H₂₃NO₃
• CAS Number: 1586038-75-6
• Molecular Weight: 301.38
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• assay: ≥98% (HPLC)
• Quality Level: 100
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: gray-green
• solubility: DMSO: 5 mg/mL
• storage temp.: −20°C

Description

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.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
KDM4

Reversible: yes

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Other Notes

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

Legal Information

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

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable