IOX1

SKU: orb1224585

Description

IOX1 is a potent, broad-spectrum inhibitor of 2OG oxygenases, including the JmjC demethylases, with IC50 of <1 uM gainst the KDM3, KDM4 and KDM6, 5-25 uM against the KDM5 and KDM2/7; IOX1 is less potent against BBOX1 (IC50=196 uM); chelates to Fe(II) in the active site of 2OG oxygenases; suppresses the proliferation and migration of vascular smooth muscle cells induced by angiotensin II.

Key Properties

• CAS Number: 5852-78-8
• MW: 189.1675
• Purity: >98% (HPLC)
• Formula: C₁₀H₇NO₃
• SMILES: O=C(C1=C2C=CC=NC2=C(O)C=C1)O
• Target: Histone Demethylase
• Solubility: DMSO: 24 mg/mL

Bioactivity

• 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. Animal model: Six-week-old male BALB/c nude mice. 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.
• 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. 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. IOX1 (50-200 μM; 2 hours) attenuates cyclin D1 and upregulates p21 mRNA levels in a concentration-dependent. IOX1 (50-200 μM; 2 hours) mediates cyclin D1 and p21 expression by regaining H3K9me3. Cell Proliferation Assay 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 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 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 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

IOX 1 | IOX-1

Quick Database Links

Gene Symbol

Histone Demethylase