IOX1
Based on 16 publication(s) in Google Scholar
IOX1, a chemical probe, is a potent broad‐spectrum inhibitor of 2OG oxygenases, including the JmjC demethylases. IOX1 inhibits KDM4C, KDM4E, KDM2A, KDM3A and KDM6B with IC50 values of 0.6 μM, 2.3 μM, 1.8 μM, 0.1 μM and 1.4 μM, respectively. IOX1 also inhibits ALKBH5.
For research use only. We do not sell to patients.
- Purity: 99.89%
- CAS No.: 5852-78-8
- Formula: C10H7NO3
- Molecular Weight:189.17
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) IOX1
More- Nat Commun. 2026 Feb 12;17(1):1214. [Abstract]
- Adv Sci (Weinh). 2024 Oct;11(40):e2309983. [Abstract]
- Cell Death Dis. 2022 Jun 13;13(6):547. [Abstract]
- Cell Death Discov. 2022 Dec 24;8(1):497. [Abstract]
- Proc Natl Acad Sci U S A. 2022 Feb 15;119(7):e2113454119. [Abstract]
- Oncogene. 2020 Apr;39(16):3336-3353. [Abstract]
- JHEP Rep. 2023 Jul 15;5(10):100849. [Abstract]
- J Agric Food Chem. 2023 Oct 18;71(41):15073-15086. [Abstract]
- Eur J Pharmacol. 2025 Feb 15:989:177247. [Abstract]
- Eur J Pharmacol. 2024 Nov 5:982:176931. [Abstract]
- Clin Exp Med. 2025 Nov 25;26(1):33. [Abstract]
- J Biol Chem. 2021 Jan-Jun:296:100121.
- Exp Cell Res. 2026 Jul 1;460(1):115042. [Abstract]
- bioRxiv. 2026 May 7.
- Research Square Preprint. 2024 Jan 18.
- Patent. US20180263995A1.
Customer Validation & Images
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RT-PCR
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WB
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In Vivo Efficacy Study
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In Vivo Efficacy Study
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In Vivo Efficacy Study
Biological Activity
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KDM2 |
KDM3 |
KDM4 |
KDM6 |
KDM3A |
KDM3B |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
48.2 μM
Compound: 5-Carboxy-8-HQ
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Cytotoxicity against human A549 cells assessed as cell viability after 48 hrs by MTT assay
Cytotoxicity against human A549 cells assessed as cell viability after 48 hrs by MTT assay
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[PMID: 26491978] |
| HCT-116 | IC50 |
28.1 μM
Compound: 5-Carboxy-8-HQ
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Cytotoxicity against human HCT116 cells assessed as cell viability after 48 hrs by MTT assay
Cytotoxicity against human HCT116 cells assessed as cell viability after 48 hrs by MTT assay
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[PMID: 26491978] |
| HeLa | EC50 |
87 μM
Compound: 69
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Inhibition of human Flag-tagged KDM4A expressed in human HeLa cells assessed as increase in H3K9me3 level after 24 hrs by DAPI staining based immunofluorescence assay
Inhibition of human Flag-tagged KDM4A expressed in human HeLa cells assessed as increase in H3K9me3 level after 24 hrs by DAPI staining based immunofluorescence assay
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[PMID: 26710088] |
| HeLa | IC50 |
86.5 μM
Compound: 211
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Inhibition of Flag-tagged JMJD2A in human HeLa cells using H3K9me3 peptide as substrate by immunofluorescence assay
Inhibition of Flag-tagged JMJD2A in human HeLa cells using H3K9me3 peptide as substrate by immunofluorescence assay
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10.1039/C1MD00199J |
| MCF7 | IC50 |
66.4 μM
Compound: 5-Carboxy-8-HQ
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Cytotoxicity against human MCF7 cells assessed as cell viability after 48 hrs by MTT assay
Cytotoxicity against human MCF7 cells assessed as cell viability after 48 hrs by MTT assay
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[PMID: 26491978] |
IOX1 (0-200 μM; 2 hours) inhibits the proliferation and migration of vascular smooth muscle cells (VSMCs) stimulated with angiotensin II (Ang II) in a concentration-dependent manner[2]. IOX1 (200 μM; 24 hours) blocks the cell cycle progression of angiotensin II (Ang II)-VSMCs by increasing the percentage of cells in the G0/G1 phase[2]. IOX1 (50-200 μM; 2 hours) attenuates cyclin D1 and upregulates p21 mRNA levels in a concentration-dependent[2]. IOX1 (50-200 μM; 2 hours) mediates cyclin D1 and p21 expression by regaining H3K9me3[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Vascular smooth muscle cells (VSMCs)
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Concentration:50 μM, 100 μM, 200 μM
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Incubation Time:Pretreated 2 hours
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Result:Exhibited a decrease in proliferation and migration.
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Cell Line:Vascular smooth muscle cells (VSMCs)
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Concentration:200 μM
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Incubation Time:24 hours
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Result:Slowed down the progression of the cell cycle from the G0/G1 to the S phase.
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Cell Line:Vascular smooth muscle cells (VSMCs)
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Concentration:50 μM, 100 μM, 200 μM
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Incubation Time:2 hours
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Result:Decreased cyclin D1 mRNA expression and increased p21 mRNA expression.
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Cell Line:Vascular smooth muscle cells (VSMCs)
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Concentration:50 μM, 100 μM, 200 μM
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Incubation Time:2 hours
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Result:Enhanced the total protein levels of H3K9me3.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Six-week-old male BALB/c nude mice[4]
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Dosage:10 mg/kg, 20 mg/kg
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Administration:12 days
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Result: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.Significantly reduced the protein levels of EpCAM and Sox9 in LCSC orthotopic graft tumors nhibited LCSC orthotopic graft tumor growth.Decreased Ki67-positive tumor cells and markedly reduced the tumorsphere formation abilities of LCSCs in a dose-dependent manner.
Chemical Information
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CAS No. 5852-78-8
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Appearance Solid
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Molecular Weight 189.17
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Formula C10H7NO3
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Color Off-white to yellow
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SMILES
O=C(C1=C2C=CC=NC2=C(O)C=C1)O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (16)
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Journal Impact Factor
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Most Recent
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Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
Adv Sci (Weinh)
KDM3A Ablation Activates Endogenous Retrovirus Expression to Stimulate Antitumor Immunity in Gastric Cancer. [Abstract]2024 Oct;11(40):e2309983. PMID: 39031630
IOX1 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Oct;11(40):e2309983. [Abstract]
qPCR analysis of CXCL10, IFNB1, and ISG15 mRNA transcripts in CTL, sgKDM3A group, and KDM3A inhibitor (IOX1) group. In hibitor group, tumor cells were pretreated with 5 µmol/mL IOX1 for 48 h.
IOX1 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Oct;11(40):e2309983. [Abstract]
Western blot showing the expression of RIG‐I, MDA5, MAVS, TBK1, phosphorylated TBK1 (ρ‐TBK1), IRF3, and ρ‐IRF3 in CTL and sgKDM3A. Inhibitor group, tumor cells were pretreated with 5 µmol/mL IOX1 for 48 h.
IOX1 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Oct;11(40):e2309983. [Abstract]
BGC823 tumor cells were inoculated into nude mice (2 × 106 cells per mouse). The KDM3A inhibitors BIX01294 (10 mg/kg) and IOX1 (12.5 mg/kg) were administered by intraperitoneal injection. Timeline of the experimental setup.
IOX1 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Oct;11(40):e2309983. [Abstract]
BGC823 tumor cells were inoculated into nude mice (2 × 106 cells per mouse). The KDM3A inhibitors BIX01294 (10 mg/kg) and IOX1 (12.5 mg/kg) were administered by intraperitoneal injection. Timeline of the experimental setup. The tumor growth of BGC823 xenografts were measured.
IOX1 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Oct;11(40):e2309983. [Abstract]
BGC823 tumor cells were inoculated into nude mice (2 × 106 cells per mouse). The KDM3A inhibitors BIX01294 (10 mg/kg) and IOX1 (12.5 mg/kg) were administered by intraperitoneal injection. Timeline of the experimental setup. The tumor weight of BGC823 xenografts were measured.
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Cell Death Dis
Histone H3K36me2 demethylase KDM2A promotes bladder cancer progression through epigenetically silencing RARRES3. [Abstract]2022 Jun 13;13(6):547. PMID: 35697678 -
Cell Death Discov
ALKBH5 promotes PD-L1-mediated immune escape through m6A modification of ZDHHC3 in glioma. [Abstract]2022 Dec 24;8(1):497. PMID: 36566230 -
Proc Natl Acad Sci U S A
TRIM14 inhibits OPTN-mediated autophagic degradation of KDM4D to epigenetically regulate inflammation. [Abstract]2022 Feb 15;119(7):e2113454119. PMID: 35145029 -
Oncogene
Inflammation-induced JMJD2D promotes colitis recovery and colon tumorigenesis by activating Hedgehog signaling. [Abstract]2020 Apr;39(16):3336-3353. PMID: 32094404 -
JHEP Rep
JMJD2D stabilises and cooperates with HBx protein to promote HBV transcription and replication. [Abstract]2023 Jul 15;5(10):100849. PMID: 37701334 -
J Agric Food Chem
Chlorogenic Acid Modulates Autophagy by Inhibiting the Activity of ALKBH5 Demethylase, Thereby Ameliorating Hepatic Steatosis. [Abstract]2023 Oct 18;71(41):15073-15086. PMID: 37805933 -
Eur J Pharmacol
Targeting the ALKBH5-NLRP3 positive feedback loop alleviates cardiomyocyte pyroptosis after myocardial infarction. [Abstract]2025 Feb 15:989:177247. PMID: 39746531 -
Eur J Pharmacol
METTL3 aggravates renal fibrogenesis in obstructive nephropathy via the miR-199a-3p/PAR4 axis. [Abstract]2024 Nov 5:982:176931. PMID: 39182553 -
Clin Exp Med
Corin: a dual inhibitor for KDM1A/HDAC1, suppresses hepatocellular carcinoma by triggering cuproptosis. [Abstract]2025 Nov 25;26(1):33. PMID: 41286164 -
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Exp Cell Res
The combinations of histone lysine demethylase inhibitors with panobinostat exert enhanced effects against head and neck cancer cells. [Abstract]2026 Jul 1;460(1):115042. PMID: 42019757 -
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Solvent & Solubility
DMSO : 13.33 mg/mL (70.47 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (11.00 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (11.00 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (311 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 5.2863 mL | 26.4313 mL | 52.8625 mL | 132.1563 mL |
| 5 mM | 1.0573 mL | 5.2863 mL | 10.5725 mL | 26.4313 mL | |
| 10 mM | 0.5286 mL | 2.6431 mL | 5.2863 mL | 13.2156 mL | |
| 15 mM | 0.3524 mL | 1.7621 mL | 3.5242 mL | 8.8104 mL | |
| 20 mM | 0.2643 mL | 1.3216 mL | 2.6431 mL | 6.6078 mL | |
| 25 mM | 0.2115 mL | 1.0573 mL | 2.1145 mL | 5.2863 mL | |
| 30 mM | 0.1762 mL | 0.8810 mL | 1.7621 mL | 4.4052 mL | |
| 40 mM | 0.1322 mL | 0.6608 mL | 1.3216 mL | 3.3039 mL | |
| 50 mM | 0.1057 mL | 0.5286 mL | 1.0573 mL | 2.6431 mL | |
| 60 mM | 0.0881 mL | 0.4405 mL | 0.8810 mL | 2.2026 mL |
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