Home Epigenetics Histone Demethylase inhibitor - JMJD inhibitor IOX1 For research use only.

IOX1

IOX1 is a potent and broad-spectrum inhibitor of 2OG oxygenases, including the JmjC demethylases. IOX1 is an inhibitor of ALKBH5.

IOX1 Chemical Structure

IOX1 Chemical Structure

CAS No. 5852-78-8

Purity & Quality Control

IOX1 Related Products

Signaling Pathway

Histone Demethylase Signaling Pathways

Histone Demethylase Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HCT116 cells Cytotoxicity assay 48 h Cytotoxicity against human HCT116 cells assessed as cell viability after 48 hrs by MTT assay, IC50=28.1 μM 26491978
human A549 cells Cytotoxicity assay 48 h Cytotoxicity against human A549 cells assessed as cell viability after 48 hrs by MTT assay, IC50=48.3 μM 26491978
human HeLa cells Function assay 72 h Induction of histone methylation in human HeLa cells assessed as H3K9me2 level after 72 hrs by immunofluorescence assay 24325601
Click to View More Cell Line Experimental Data

Biological Activity

Description IOX1 is a potent and broad-spectrum inhibitor of 2OG oxygenases, including the JmjC demethylases. IOX1 is an inhibitor of ALKBH5.
Features Cell-permeant, broad-spectrum 2OG oxygenase inhibitor.
Targets
KDM3A [1]
(Cell-free assay)		 KDM4C [1]
(Cell-free assay)		 KDM6B [1]
(Cell-free assay)		 KDM2A [1]
(Cell-free assay)		 KDM4E [1]
(Cell-free assay)		 Click to View More Targets
0.1 μM 0.6 μM 1.6 μM 1.8 μM 2.3 μM
In vitro
In vitro

IOX1 increases H3K9me3 levels in HeLa cells via KDM4A inhibition without significant effect on cell viability. IOX1 shows lower efficacy in HeLa cells due to low cell permeability, while the n-octyl ester derivative improves its cell permeability. [1]
Kinase Assay AlphaScreen Assay
All reagents are diluted in 50 mM HEPES, 0.1% BSA, pH 7.5 supplemented with 0.01% Tween20 and allowed to equilibrate to room temperature prior to addition to plates. Catalytic turnover assays are run in 10 μL volumes in lowvolume 384-well plates at RT. The reaction consisted of enzyme (5 nM), biotinylated substrate peptide (30 nM), Fe(II) (1 μM), ascorbate (100 μM), 2OG (10 μM) and run at RT. For PHD2, the reaction consisted of enzyme (5 nM), biotinylated substrate peptide (60nM), Fe(II) (20 μM), ascorbate (200 μM), 2OG (2 μM) and run at RT. EDTA is used to quench the reaction (5 μL), AlphaScreen donor (Streptavidin-conjugated) and acceptor (Protein A-conjugated) beads preincubated with peptide product antibodies are added (5 μL). Plates are foil-sealed to protect from light, incubated at room temperature for 60 minutes and read on a PHERAstar FS plate reader using an AlphaScreen 680 excitation/570 emission filter set. The final bead concentration in 20 μL reaction is 20 μg/mL. IC50 values are calculated in Prism 6 after normalisation against corresponding DMSO controls.
Cell Research Cell lines HeLa cells
Concentrations ~300 μ M
Incubation Time 24 hours
Method

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.

Chemical Information & Solubility

Molecular Weight 189.17 Formula

C10H7NO3
CAS No. 5852-78-8 SDF Download IOX1 SDF
Smiles C1=CC2=C(C=CC(=C2N=C1)O)C(=O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 37 mg/mL ( (195.59 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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