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IOX1

Catalog No. T6545 CAS 5852-78-8

IOX1 is the most effective broad-spectrum 2OG oxygenases(including the JmjC demethylases) inhibitor. The IC50 of IOX1 for KDM4A, KDM3A, is 0.6 and 0.1 uM, respectively.

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IOX1, CAS 5852-78-8

Pack Size	Availability	Price/USD
2 mg	In stock	$ 38.00
5 mg	In stock	$ 61.00
10 mg	In stock	$ 90.00
25 mg	In stock	$ 198.00
50 mg	In stock	$ 328.00
100 mg	In stock	$ 487.00
1 mL * 10 mM (in DMSO)	In stock	$ 67.00

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Purity: 99.38%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	IOX1 is the most effective broad-spectrum 2OG oxygenases(including the JmjC demethylases) inhibitor. The IC50 of IOX1 for KDM4A, KDM3A, is 0.6 and 0.1 uM, respectively.
Targets&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.
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 (60 nM), 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	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)

Molecular Weight	189.17
Formula	C10H7NO3
CAS No.	5852-78-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (165.31 mM)

References and Literature

1. Schiller R, et al. ChemMedChem. 2014, 9(3), 566-571. 2. Huang Y, Su R, Sheng Y, et al. Small-molecule targeting of oncogenic FTO demethylase in acute myeloid leukemia[J]. Cancer Cell. 2019, 35(4): 677-691. e10.

Citations

1. Huang Y, Su R, Sheng Y, et al. Small-molecule targeting of oncogenic FTO demethylase in acute myeloid leukemia. Cancer Cell. 2019, 35(4): 677-691. e10.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Epigenetics Compound Library NO PAINS Compound Library Histone Modification Compound Library Bioactive Compound Library Stem Cell Differentiation Compound Library Anti-Aging Compound Library Methylation Compound Library Chromatin Modification Compound Library Bioactive Compounds Library Max

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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 add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

IOX1 5852-78-8 Chromatin/Epigenetic Histone Demethylase Inhibitor inhibit IOX-1 IOX 1 inhibitor

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