2. Epigenetics
  3. Histone Demethylase
  4. IOX1

IOX1 

Cat. No.: HY-12304 Purity: 99.72%
COA Handling Instructions

IOX1, 5-Carboxy-8-hydroxyquinoline, 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.

IOX1 Chemical Structure

IOX1 Chemical Structure

CAS No. : 5852-78-8

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Free Sample (0.1 - 0.5 mg)   Apply Now  
Solution
10 mM * 1 mL in DMSO USD 85 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 85 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 77 In-stock
Estimated Time of Arrival: December 31
10 mg USD 132 In-stock
Estimated Time of Arrival: December 31
50 mg USD 528 In-stock
Estimated Time of Arrival: December 31
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200 mg   Get quote  

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Customer Review

Based on 6 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

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Description

IOX1, 5-Carboxy-8-hydroxyquinoline, 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[1][2]. IOX1 also inhibits ALKBH5[3].

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].

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].

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

Appearance

Solid

Formula

C10H7NO3
CAS No.
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 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 13.33 mg/mL (70.47 mM; Need ultrasonic and warming)

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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.72%

COA (254 KB) HNMR (254 KB) LCMS (90 KB)

Handling Instructions (2659 KB)
References
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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.

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The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
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Keywords:

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

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