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IOX1

Name: IOX1
Brand: Selleck Chemicals
SKU: S7234
Rating: 5 (14 reviews)

Catalog No.S7234 Purity:99.98%

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

IOX1 Chemical Structure

CAS No. 5852-78-8

Purity & Quality Control

Batch: Purity: 99.98%

99.98

IOX1 Related Products

Related Targets	KDM1 KDM2 KDM3 KDM4 KDM5 KDM6	Click to Expand
Related Products	GSK J4 HCl SP2509 CPI-455 HCl Iadademstat (ORY-1001) 2HCl GSK-LSD1 2HCl JIB-04 OG-L002 ML324 GSK J1 CP2 CPI-455	Click to Expand
Related Compound Libraries	Kinase Inhibitor Library FDA-approved Drug Library Natural Product Library Bioactive Compound Library-I Highly Selective Inhibitor Library	Click to Expand

Signaling Pathway

Histone Demethylase Signaling Pathway

Cell Data

Cell Lines	Assay Type	Incubation Time	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	Click to View More Targets

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
Kinase 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.

References

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)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

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

Water : Insoluble

Ethanol : Insoluble

Molecular Weight Calculator

In vivo Batch: Add solvents to the product individually and in order.				In vivo Formulation Calculator
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.000mg/ml (15.86mM)	Taking the 1 mL working solution as an example, add 50 μL of 60 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.000mg/ml (15.86mM)	Taking the 1 mL working solution as an example, add 50 μL of 60 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

Preparing Stock Solutions

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

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