IOX1

Name: IOX1
Brand: MedChemExpress
SKU: HY-12304
Rating: 5.0 (14 reviews)

Cat. No.: HY-12304 Purity: 99.89%: Data Sheet
COA

SDS
Handling Instructions
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Technical Support

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.

CAS No. : 5852-78-8

Size	Stock	Quantity

Free Sample (0.1 - 0.2 mg)	Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	Get quote
200 mg	Get quote

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Customer Review

Based on 14 publication(s) in Google Scholar

14 Publications Citing Use of MCE IOX1

RT-PCR

In Vivo Efficacy Study

: IOX1 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Jul 19: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 Jul 19: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 Jul 19: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 Jul 19: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 Jul 19: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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View All Isoforms

KDM1/LSD1 KDM2 KDM3 KDM4 KDM5 KDM6 KDM7

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

KDM2

KDM3

KDM4

KDM6

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	48.2 3 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]
A549	IC₅₀	48.2 3 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 3 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]
HCT-116	IC₅₀	28.1 3 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 3 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 3 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
HeLa	IC₅₀	86.5 3 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
A549	IC₅₀	48.2 3 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]
HeLa	EC₅₀	87 3 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]
MCF7	IC₅₀	66.4 3 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]
MCF7	IC₅₀	66.4 3 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]
HCT-116	IC₅₀	28.1 3 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 3 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 3 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 3 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.

Molecular Weight

189.17

Formula

C₁₀H₇NO₃

CAS No.

5852-78-8

Appearance

Solid

Color

Off-white to yellow

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the 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.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

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

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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

Purity: 99.89%

Select Batch:

Data Sheet (284 KB) SDS (393 KB)

COA (254 KB) HNMR (113 KB) LCMS (140 KB)

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]

[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

Complete Stock Solution Preparation Table

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

IOX1 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

IOX15852-78-8IOX 1IOX-1Histone DemethylaseInhibitorinhibitorinhibit

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IOX1

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IOX1 Related Antibodies

14 Publications Citing Use of MCE IOX1

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View All Histone Demethylase Isoform Specific Products:

Biological Activity

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References

Customer Review

IOX1 Related Antibodies

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Complete Stock Solution Preparation Table

IOX1 Related Classifications

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