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IOX1 Histone Demethylase inhibitor

Name: IOX1
Brand: Selleck Chemicals
SKU: S7234
Availability: InStock
Rating: 5 (15 reviews)

Cat.No.S7234

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

Chemical Structure

Molecular Weight: 189.17

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.98%

99.98

Related Targets	Epigenetic Reader Domain HDAC JAK Histone Methyltransferase AMPK PKC PARP HIF Histone Acetyltransferase Aurora Kinase Sirtuin PRMT EZH1/2 DNA Methyltransferase Pim LSD1 MLL JMJD G9a/GLP NSD FTO MicroRNA PAD SETD SMYD DOT1 COMT WDR5 HNMT SAM MTase
Related Products	GSK-J4 Hydrochloride SP2509 CPI-455 HCl Ladademstat (ORY-1001) Dihydrochloride GSK-LSD1 2HCl JIB-04 OG-L002 ML324 GSK J1 CP2 CPI-455 KDM5-IN-1 NCGC00244536 GSK467 JARID1B Antibody [A10D8] Zavondemstat PFI-90 TC-E5002(KDM2/7-IN-1) AS-8351 KDM4D-IN-1 GSK-J4 JMJD2A Antibody [B12L5] KDM6A/UTX Antibody [J23B17] PBIT Z-JIB-04 (NSC 693627) KDM2A Antibody [B7P10] Daminozide JNJ-9350

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Incubation Time	Activity Description
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
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
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
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	189.17	Formula	C₁₀H₇NO₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	5852-78-8	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	C1=CC2=C(C=CC(=C2N=C1)O)C(=O)O

Solubility

In vitro
Batch:

DMSO : 37 mg/mL (195.59 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
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.

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.

Mechanism of Action

Features	Cell-permeant, broad-spectrum 2OG oxygenase inhibitor.
Targets/IC₅₀/Ki	KDM3A ^[1] (Cell-free assay) 0.1 μM KDM4C ^[1] (Cell-free assay) 0.6 μM KDM6B ^[1] (Cell-free assay) 1.6 μM KDM2A ^[1] (Cell-free assay) 1.8 μM KDM4E ^[1] (Cell-free assay) 2.3 μM KDM5C ^[1] (Cell-free assay) 19 μM PHD2 ^[1] (Cell-free assay) 33 μM
In vitro	IOX1 increases H3K9me3 levels in HeLa cells via KDM4A inhibition without significant effect on cell viability. This compound 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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/24504543/ [2] https://pubmed.ncbi.nlm.nih.gov/34879293/

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