Name | 5-Carboxy-8-hydroxyquinoline |
Synonyms | IOX1 5-Carboxy-8-hydroxyquinoline JMJD2 Inhibitor, 5-carboxy-8HQ 8-Hydroxyquinoline-5-carboxylic Acid 8-hydroxy-5-Quinolinecarboxylic acid |
CAS | 5852-78-8 |
InChIKey | JGRPKOGHYBAVMW-UHFFFAOYSA-N |
Molecular Formula | C10H7NO3 | |
Molar Mass | 189.17 | |
Density | 1.480±0.06 g/cm3(Predicted) | |
Melting Point | 301 °C (decomp) | |
Boling Point | 464.5±30.0 °C(Predicted) | |
Solubility | DMSO: soluble10mg/mL, clear | |
Appearance | powder | |
Color | white to brown | |
pKa | 1.82±0.10(Predicted) | |
Storage Condition | 2-8°C | |
Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months. | |
Physical and Chemical Properties |
|
Hazard Symbols | Xn - Harmful |
Risk Codes | 22 - Harmful if swallowed |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 5.286 ml | 26.431 ml | 52.863 ml |
5 mM | 1.057 ml | 5.286 ml | 10.573 ml |
10 mM | 0.529 ml | 2.643 ml | 5.286 ml |
5 mM | 0.106 ml | 0.529 ml | 1.057 ml |
biological activity | IOX1, is a potent broad-spectrum inhibitor of 2og oxygenases, including JmjC norenzymes. IOX1 inhibited 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 inhibits alkbh5. |
Cell Line: | Vascular smooth muscle cells (VSMCs) Vascular smooth muscle cells (VSMCs) Vascular smooth muscle cells (VSMCs) Vascular smooth muscle cells (VSMCs) |
Concentration: | 50 μM, 100 μM, 200 μM 200 μM 50 μM, 100 μM, 200 μM 50 μM, 100 μM, 200 μM |
Incubation Time: | Pretreated 2 hours 24 hours 2 hours 2 hours |
Result: | Exhibited a decrease in proliferation and migration. Slowed down the progression of the cell cycle from the G0/G1 to the S phase. Decreased cyclin D1 mRNA expression and increased p21 mRNA expression. Enhanced the total protein levels of H3K9me3. 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. |
Animal Model: | Six-week-old male BALB/c nude mice |
Dosage: | 10 mg/kg, 20 mg/kg |
Administration: | 12 days |