IOX1

製品コードS7234 バッチS723402

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₁₀H₇NO₃

分子量

189.17

CAS No.

5852-78-8

Solubility (25°C)*

体外

DMSO

37 mg/mL (195.59 mM)

Water

Insoluble

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

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 この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	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 この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	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.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	IOX1は、JmjC デメチラーゼを含む2OG 酸素添加酵素の強力で広範囲な阻害剤です。IOX1はALKBH5の阻害剤です。
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.
特徴	Cell-permeant, broad-spectrum 2OG oxygenase inhibitor.

プロトコル(参考用のみ)

キナーゼアッセイ	AlphaScreen Assay
キナーゼアッセイ	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.
細胞アッセイ	細胞株	HeLa cells
	濃度	~300 μ M
	反応時間	24 hours
	実験の流れ	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.

参考

https://pubmed.ncbi.nlm.nih.gov/24504543/
https://pubmed.ncbi.nlm.nih.gov/34879293/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

HIF-independent oxygen sensing via KDM6A regulates ferroptosis [ Mol Cell, 2025, 85(15):2973-2987.e6]	PubMed: 40712585
Methylstat sensitizes ovarian cancer cells to PARP-inhibition by targeting the histone demethylases JMJD1B/C [ Cancer Gene Ther, 2025, 10.1038/s41417-025-00874-z]	PubMed: 39915607
Characterization of the m6A regulators' landscape highlights the clinical significance of acute myocardial infarction [ Front Immunol, 2024, 15:1308978]	PubMed: 38571952
ALKBH5 insufficiency protects against ferroptosis-driven cisplatin-induced renal cytotoxicity [ Cell Biol Toxicol, 2024, 40(1):99]	PubMed: 39557743
Inhibition of ALKBH5 attenuates I/R-induced renal injury in male mice by promoting Ccl28 m6A modification and increasing Treg recruitment [ Nat Commun, 2023, 14(1):1161]	PubMed: 36859428
Oxygen-sensitive methylation of ULK1 is required for hypoxia-induced autophagy [ Nat Commun, 2022, 13(1):1172]	PubMed: 35246531
Discovery of two novel ALKBH5 selective inhibitors that exhibit uncompetitive or competitive type and suppress the growth activity of glioblastoma multiforme [ Chem Biol Drug Des, 2022, 10.1111/cbdd.14051]	PubMed: 35384315
IOX1 activity as sepsis therapy and an antibiotic against multidrug-resistant bacteria [ Sci Rep, 2021, 11(1):2942]	PubMed: 33536477
IOX1 impedes host inflammation in imiquimod-triggered psoriasis [ Heliyon, 2021, 7(11):e08433]	PubMed: 34877426
KDM3A Senses Oxygen Availability to Regulate PGC-1α-Mediated Mitochondrial Biogenesis. [ Mol Cell, 2019, 76(6):885-895]	PubMed: 31629659

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。