IOX1

SKU: orb1300673

Description

IOX1 is a potent broad-spectrum inhibitor of 2-oxoglutarate-dependent oxygenases, including JmjC histone demethylases such as KDM4A (IC50 0.6 µM) and KDM3A (IC50 0.1 µM). It is widely used in biochemical and cellular research to probe epigenetic mechanisms and has been applied in both in vitro and in vivo studies investigating cancer and other diseases.

Research Area

Epigenetics & Chromatin

Key Properties

• CAS Number: 5852-78-8
• MW: 189.17
• Purity: 99.67% (May vary between batches)
• Formula: C₁₀H₇NO₃
• SMILES: OC(=O)c1ccc(O)c2ncccc12
• Target: Histone Demethylase
• Solubility: DMSO:50 mg/mL (264.31 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (10.57 mM)

Bioactivity

• Target IC50:
  KDM4A:0.6 uM|KDM3A:0.1 uM
• In Vitro:
  IOX1with an in vitro IC50 value in the micromolar range is the most effective against a representative panel of 2OG oxygenases, including non-JmjC 2OG oxygenases. In HeLa cells, however, its IC50 is 86uM, which efficacy is about a hundred-fold lower, possibly because of low cell permeability resulting from its polar C-5 carboxyl group.
• Cell Research:
  Antiproliferative activities of compounds are determined by the MTT assay. HeLa cells are seeded into 96-well plates and cultured at 37 °C for 24 h to achieve 70%. Subsequently, the medium is replaced with DMEM medium containing the tested compounds in different concentrations of 1-300 μM in 1% DMSO. Staurosporine in 0.03-10 μM final concentration is used as a control for cytotoxicity. After 24 h of treatment, the medium is replaced with CellTiter 96 Aqueous One Solution Reagent and incubated for 4 hours. CC50 values are calculated in Prism 6 software after normalisation against corresponding 1% DMSO treated cells and 1% DMSO in media (no cells) controls.(Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

JMJC demethylase, IOX 1, IOX1, IOX-1, inhibit, Inhibitor, KDM4A/KDM3A, Histone Demethylase, HistoneDemethylase

Compound Identifiers

PubChem CID

459617