Art. -Nr.: HY-12304

IOX1

16 Cited Publications

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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.

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Reinheit: 99.89%
CAS. Nr.: 5852-78-8
Formel: C₁₀H₇NO₃
Molecular Weight:189.17

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

IOX1 Chemical Structure

CAS. Nr.: 5852-78-8

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (16)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

KDM2

KDM3

KDM4

KDM6

KDM3A

KDM3B

Alle Histone Demethylase Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	48.2 μM Compound: 5-Carboxy-8-HQ	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	[PMID: 26491978]
HCT-116	IC₅₀	28.1 μM Compound: 5-Carboxy-8-HQ	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	[PMID: 26491978]
HeLa	EC₅₀	87 μM Compound: 69	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	[PMID: 26710088]
HeLa	IC₅₀	86.5 μM Compound: 211	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	10.1039/C1MD00199J
MCF7	IC₅₀	66.4 μM Compound: 5-Carboxy-8-HQ	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	[PMID: 26491978]

In Vitro

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.

Cell Proliferation Assay^[2]

Cell Line:

Vascular smooth muscle cells (VSMCs)
Concentration:

50 μM, 100 μM, 200 μM
Incubation Time:

Pretreated 2 hours
Result:

Exhibited a decrease in proliferation and migration.

Cell Cycle Analysis^[2]

Cell Line:

Vascular smooth muscle cells (VSMCs)
Concentration:

200 μM
Incubation Time:

24 hours
Result:

Slowed down the progression of the cell cycle from the G0/G1 to the S phase.

RT-PCR^[2]

Cell Line:

Vascular smooth muscle cells (VSMCs)
Concentration:

50 μM, 100 μM, 200 μM
Incubation Time:

2 hours
Result:

Decreased cyclin D1 mRNA expression and increased p21 mRNA expression.

RT-PCR^[2]

Cell Line:

Vascular smooth muscle cells (VSMCs)
Concentration:

50 μM, 100 μM, 200 μM
Incubation Time:

2 hours
Result:

Enhanced the total protein levels of H3K9me3.

In Vivo

IOX1 (5-c-8HQ) (oral gavage; 10-20 mg/kg; 12 days) inhibits tumor growth and attenuates the self-renewal of liver cancer stem-like cells (LCSCs) in vivo^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Six-week-old male BALB/c nude mice^[4]
Dosage:

10 mg/kg, 20 mg/kg
Administration:

12 days
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

CAS. Nr. 5852-78-8
Appearance Solid
Molecular Weight 189.17
Formel C₁₀H₇NO₃
Color Off-white to yellow
SMILES

O=C(C1=C2C=CC=NC2=C(O)C=C1)O
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (16)

All RT-PCRWBIn Vivo Efficacy Study

Sort by:

Journal Impact Factor

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.
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
J Biol Chem

2021 Jan-Jun:296:100121. PMID: 33234596
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
bioRxiv

2026 May 7.
Research Square Preprint

2024 Jan 18.
Patent

US20180263995A1.

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (311 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

[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

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

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IOX1

Chemical Probe Library

Anti-Cancer Metabolism Compound Library

Transcription Factor-Targeted Library

Heterocyclic Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Methylation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Epigenetics Compound Library Mini

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Publications Citing Use of MedChemExpress (MCE) IOX1

Alle Histone Demethylase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (16)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

IOX1

Chemical Probe Library

Anti-Cancer Metabolism Compound Library

Transcription Factor-Targeted Library

Heterocyclic Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Methylation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Epigenetics Compound Library Mini

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Publications Citing Use of MedChemExpress (MCE) IOX1

Alle Histone Demethylase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (16)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

IOX1 Related Classifications

HY-12304 Related Classifications