IOX 1 |
カタログ番号GC17754
One-Click Copy Product Info
|
IOX 1、5-カルボキシ-8-ヒドロキシキノリンは、JmjC デメチラーゼを含む 2OG オキシゲナーゼの強力な広域スペクトル阻害剤です。 IOX 1 は、KDM4C、KDM4E、KDM2A、KDM3A、および KDM6B を、それぞれ 0.6 μM、2.3 μM、1.8 μM、0.1 μM、および 1.4 μM の IC50 値で阻害します。 IOX 1 は ALKBH5 も阻害します。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 5852-78-8
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
IOX 1 is a potent broad‐spectrum inhibitor of 2OG oxygenases, which inhibits KDM4C, KDM4E, KDM2A, KDM3A and KDM6B with IC50 values of 0.6μM, 2.3μM, 1.8μM, 0.1μM and 1.4μM, respectively [1]. IOX 1 can increase the level of histone H3 methylation, inhibit the expression of matrix metalloproteinases, N-cadherin and vimentin, thereby suppressing the invasion of cancer cells [2]. IOX 1 has been widely used to reduce the proliferation of acute myeloid leukemia cells and regulate the DNA damage pathway [3].
In vitro, IOX 1 treatment for 2h (200μM) significantly inhibited the proliferation and migration of vascular smooth muscle cells (VSMCs) induced by Ang II [4]. Treatment of N-WASP-deficient keratinocytes with 200μM IOX 1 for 24 hours can restore the expression of H3K9me2 and IL-23A [5]. Treatment with 100μM IOX 1 for 72 hours impaired proliferation of B cells in mouse spleens and suppressed cyclin E1 expression [6].
In vivo, IOX 1 treatment via intragastrical administration at a dose of 20mg/kg/day for 12 days reduced cardiomyocyte apoptosis and decreased the mRNA and protein expression levels of p53 and Bax in a mouse model of myocardial infarction (MI)[7].
References:
[1] Schiller R, Scozzafava G, Tumber A, et al. A cell‐permeable ester derivative of the JmjC histone demethylase inhibitor IOX1[J]. ChemMedChem, 2014, 9(3): 566-571.
[2] Chang S L Y, Lee C W, Yang C Y, et al. IOX-1 suppresses metastasis of osteosarcoma by upregulating histone H3 lysine trimethylation[J]. Biochemical Pharmacology, 2023, 210: 115472.
[3] Monaghan L, Bunschoten R P, Bittencourt‐Silvestre J, et al. Selective small molecule targeting of KDM4 as a therapeutic strategy to reduce proliferation of acute myeloid leukaemia[J]. British Journal of Haematology, 2026.
[4] Hu Q I, Chen J, Zhang J, et al. IOX1, a JMJD2A inhibitor, suppresses the proliferation and migration of vascular smooth muscle cells induced by angiotensin II by regulating the expression of cell cycle-related proteins[J]. International journal of molecular medicine, 2016, 37(1): 189-196.
[5] Li H, Yao Q, Mariscal A G, et al. Epigenetic control of IL-23 expression in keratinocytes is important for chronic skin inflammation[J]. Nature communications, 2018, 9(1): 1420.
[6] Jiang Y, Li C, Wu Q, et al. Iron-dependent histone 3 lysine 9 demethylation controls B cell proliferation and humoral immune responses[J]. Nature communications, 2019, 10(1): 2935.
[7] Shen C, Chen X, Lin Y, et al. Hypoxia triggers cardiomyocyte apoptosis via regulating the m6A methylation-mediated LncMIAT/miR-708-5p/p53 axis[J]. Heliyon, 2024, 10(11).
| Cell experiment [1]: | |
|
Cell lines |
Vascular smooth muscle cells (VSMCs) |
|
Preparation Method |
VSMCs were cultured in DMEM supplemented with 10% fetal bovine serum (FBS) and 1% penicillin/streptomycin in an atmosphere of 5% CO2, at 37°C. Approximately 8000 VSMCs were seeded in 96-well plates in 200µl of culture medium. Following synchronization with DMEM containing 0.1% FBS for 24h, the VSMCs were pretreated with IOX 1 at various concentrations (0, 50, 100 and 200µM) for 2h, and then stimulated with 1µM Ang II for 24h. The cell proliferation was evaluated. |
|
Reaction Conditions |
0, 50, 100 and 200µM; 2h |
|
Applications |
IOX 1 treatment significantly reduced cell proliferation of VSMCs induced by Ang II in a dose-dependent manner. |
| Animal experiment [2]: | |
|
Animal models |
Male C57BL/6 mice |
|
Preparation Method |
Male C57BL/6 mice (8 weeks old) were given free access to water and food, and were housed in a room at a controlled temperature and humidity with a 12-h light/dark cycle. MI mouse model was induced by ligating the left anterior descending (LAD). Before the operation, the mice in the sham and MI groups were intragastrically administered 0.9% sodium chloride solution, whereas mice in the MI + IOX 1 group were intragastrically administered the IOX 1, at a dose of 20mg/kg/day for 12 days. Collect the heart tissues of mice for analysis. |
|
Dosage form |
20mg/kg/day for 12 days; i.g. |
|
Applications |
IOX 1 treatment reduced cardiomyocyte apoptosis and decreased the mRNA and protein expression levels of p53 and Bax in a mouse model of MI. |
|
References: |
|
| Cas No. | 5852-78-8 | SDF | |
| Chemical Name | 8-hydroxyquinoline-5-carboxylic acid | ||
| Canonical SMILES | OC1=C2N=CC=CC2=C(C(O)=O)C=C1 | ||
| Formula | C10H7NO3 | M.Wt | 189.17 |
| 溶解度 | ≥ 5.75mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 5.2863 mL | 26.4313 mL | 52.8625 mL |
| 5 mM | 1.0573 mL | 5.2863 mL | 10.5725 mL |
| 10 mM | 528.6 μL | 2.6431 mL | 5.2863 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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.)
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 saline, 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.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >97.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 14 reference(s) in Google Scholar.)