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Purity: ≥98%
IOX1 (5-Carboxy-8-hydroxyquinoline) is a novel, potent and broad-spectrum inhibitor of 2OG oxygenases (e.g. JMJD and JmjC demethylases) with anticancer activity. In MALDI-TOF MS assay, IOX 1 inhibited JMJD2E, JMJD2A, FIH and PHD2 with IC50 values of 2.4, 1.7, 20.5 and 14.3 μM, respectively. In HeLa cells, IOX 1 increased H3K9me3 fluorescence intensity, suggesting that IOX 1 inhibited H3K9me3 demethylation induced by JMJD2A with IC50 value of 86.5 μM.
| ln Vitro |
In a concentration-dependent manner, IOX1 (0-200 μM; 2 hours) suppresses the migration and proliferation of vascular smooth muscle cells (VSMCs) induced with angiotensin II (Ang II)[2]. IOX1 (200 μM; 24 hours) increases the proportion of cells in the G0/G1 phase, which prevents angiotensin II (Ang II)-VSMCs from progressing through the cell cycle[2]. IOX1 (50-200 μM; 2 hours) in a concentration-dependent manner attenuates cyclin D1 and upregulates p21 mRNA levels[2]. IOX1 (50-200 μM; 2 hours) restores H3K9me3, which mediates cyclin D1 and p21 expression[2].
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| ln Vivo |
In vivo, IOX1 (5-c-8HQ) (oral gavage; 10–20 mg/kg; 12 days) attenuates the self-renewal of liver cancer stem-like cells (LCSCs) and suppresses tumor growth[1].
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| Animal Protocol |
Animal/Disease Models: Sixweeks old male BALB/c nude mice[4]
Doses: 10 mg/kg, 20 mg/kg Route of Administration: 12 days Experimental Results: Did not result in obvious adverse effects on mice as demonstrated by no body weight reduction and no toxicity to the major organs after treatment. Inhibited LCSC orthotopic graft tumor growth. Dramatically decreased the protein levels of EpCAM and Sox9 in LCSC orthotopic graft tumors nhibited LCSC orthotopic graft tumor growth. diminished Ki67-positive tumor cells and markedly decreased the tumorsphere formation abilities of LCSCs in a dose-dependent manner. |
| References |
[1]. Schiller R, et al. A cell-permeable ester derivative of the JmjC histone demethylase inhibitor IOX1. ChemMedChem. 2014 Mar;9(3):566-71.
[2]. Hu Q, 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. Int J Mol Med. 2016 Jan;37(1):189-96. [3]. Li F, et al. A Radioactivity-Based Assay for Screening Human m6A-RNA Methyltransferase, METTL3-METTL14 Complex, and Demethylase ALKBH5. Biomol Screen. 2016 Mar;21(3):290-7. [4]. Yuan Deng, et al. Histone demethylase JMJD2D promotes the self-renewal of liver cancer stem-like cells by enhancing EpCAM and Sox9 expression. J Biol Chem |
| Molecular Formula |
C10H7NO3
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| Molecular Weight |
189.17
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| CAS # |
5852-78-8
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| Related CAS # |
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| SMILES |
O([H])C1C([H])=C([H])C(C(=O)O[H])=C2C([H])=C([H])C([H])=NC2=1
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| InChi Key |
JGRPKOGHYBAVMW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C10H7NO3/c12-8-4-3-7(10(13)14)6-2-1-5-11-9(6)8/h1-5,12H,(H,13,14)
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| Chemical Name |
8-Hydroxyquinoline-5-carboxylic acid
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Preparing Stock Solutions | 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 | 0.5286 mL | 2.6431 mL | 5.2863 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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