IOX2
IOX2
CAS: 931398-72-0
Molecular Formula: C19H16N2O5
IOX2 - Names and Identifiers
IOX2 - Physico-chemical Properties
| Molecular Formula | C19H16N2O5 |
| Molar Mass | 352.34 |
| Density | 1.470±0.06 g/cm3(Predicted) |
| Boling Point | 642.8±55.0 °C(Predicted) |
| Solubility | DMSO: soluble5mg/mL, clear (warmed) |
| Appearance | powder |
| Color | white to beige |
| pKa | 3.61±0.10(Predicted) |
| Storage Condition | 2-8°C |
| In vitro study | LOX2 potently inhibited PHD2 (IC50 of 21 nM), more than 100-fold more selective than JMJD2A, JMJD2C, JMJD2E, JMJD3, or 2OG oxygenase FIH(IC50<100 μm). LOX2 effectively acts on the cells, and at 50 μm, it acts on RCC4 cells to inhibit HIF-1α hydroxylation. Hypoxia-inducible factor (HIF) is regulated by the hydroxylation of prolyl residues in the oxygen-dependent degradation domain at the HIF-1α subunit. 1, 2 HIF prolyl hydroxylation is mediated by prolyl hydroxylase domain enzymes (PHD1, 2, and 3), Fe(II) and 2-oxoglutarate (2og). A member of the oxygenase family catalyzes. They require molecular oxygen as a co-substrate, thus acting as a hypoxia-sensitive element of the HIF system. Hypoxia inhibits PHD activity and increases the abundance and activity of HIF transcription complexes. IOX2 potently inhibits PHD2 (IC50 of 21 nM), more than 100-fold more selective than inhibiting JMJD2A, JMJD2C, JMJD2E, JMJD3, or 2OG oxygenase FIH(IC50<100 μm). LOX2 effectively acts on the cells, and at 50 μm, it acts on RCC4 cells to inhibit HIF-1α hydroxylation. Hypoxia-inducible factor (HIF) is regulated by the hydroxylation of prolyl residues in the oxygen-dependent degradation domain at the HIF-1α subunit. 1, 2 HIF prolyl hydroxylation is produced by prolyl hydroxylase domain enzymes (PHD1, 2, and 3), Fe(II) and 2-ketoglutarate A member of the (2OG) oxygenase family catalyzes. They require molecular oxygen as a co-substrate, thus acting as a hypoxia-sensitive element of the HIF system. Hypoxia inhibits PHD activity and increases the abundance and activity of HIF transcription complexes. |
| In vivo study | To investigate the utility of IOX2 as in vivo functional probes, IOX2 is tested to upregulate HIF signaling in a whole organism, that is, transgenic zebrafish ( Danio rerio ). Because the expression of the PHD3 encoding gene is regulated by HIF in humans and zebrafish, PHD3 levels are a readout of HIF activity. A zebrafish hypoxia reporter line is generated expressing GFP with the phd3 promoter elements. Transgenic wild-type embryos at 3 days postfertilization treated with compounds (10 μM) for 2 days displayed clear increase in phd3:EGFP expression in the liver, relative to controls. Significant increases in GFP levels are observed with IOX2. |
IOX2 - Risk and Safety
| Hazard Symbols | T - Toxic |
| Risk Codes | 25 - Toxic if swallowed |
| Safety Description | 45 - In case of accident or if you feel unwell, seek medical advice immediately (show the label whenever possible.) |
| UN IDs | UN 2811 6.1 / PGIII |
| WGK Germany | 3 |
IOX2 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.838 ml | 14.191 ml | 28.382 ml |
| 5 mM | 0.568 ml | 2.838 ml | 5.676 ml |
| 10 mM | 0.284 ml | 1.419 ml | 2.838 ml |
| 5 mM | 0.057 ml | 0.284 ml | 0.568 ml |
Last Update：2024-01-02 23:10:35
IOX2 - Reference Information
| biological activity | IOX2 is an effective HIF-1α prolyl hydroxylase-2 (PHD2)(HIF-1α prolyl hydroxylase-2) inhibitor, IC50 is 21 nM, which is more than 100 times more selective than acting on JMJD2A, JMJD2C, JMJD2E, JMJD3 and 2OG oxygen synthase FIH. IOX2 (JICL38) is an effective inhibitor of HIF-1α prolyl hydroxylase-2 (PHD2). IC50 is 21 nM in cell-free test, which is more than 100 times higher than FIH selectivity for JMJD2A,JMJD2C,JMJD2E,JMJD3 and 2OG oxygenase. |
| in vitro study | IOX2 effectively inhibits PHD2 (IC50 is 21 nM), which is more than 100 times more selective than inhibiting JMJD2A, JMJD2C, JMJD2E, JMJD3, or 2OG oxygenase FIH(IC50<100 μM). IOX2 effectively acts on cells. At 50 μM, IOX2 acts on RCC4 cells to inhibit HIF-1α hydroxylation. Hypoxia-inducible factor (HIF) is regulated by hydroxylation of prolyl residues in oxygen-dependent degradation domains in the HIF-1α subunit. 1, 2 HIF prolyl hydroxylation is catalyzed by members of the prolyl hydroxylase domain enzymes (PHD1, 2, and 3), Fe(II), and 2-ketoglutarate (2OG) oxygenase family. They require molecular oxygen as an auxiliary substrate, thus acting as an anoxic sensitive element of the HIF system. Hypoxia inhibits PHD activity and increases the abundance and activity of HIF transcription complexes. IOX2 is effective in inhibiting PHD2 (IC50 is 21 nM), which is more than 100 times more selective than inhibiting JMJD2A, JMJD2C, JMJD2E, JMJD3, or 2OG oxygenase FIH(IC50<100 μM). IOX2 effectively acts on cells. At 50 μM, IOX2 acts on RCC4 cells to inhibit HIF-1α hydroxylation. Hypoxia-inducible factor (HIF) is regulated by hydroxylation of prolyl residues in oxygen-dependent degradation domains in the HIF-1α subunit. 1, 2 HIF prolyl hydroxylation is catalyzed by members of the prolyl hydroxylase domain enzymes (PHD1, 2, and 3), Fe(II), and 2-ketoglutarate (2OG) oxygenase family. They require molecular oxygen as an auxiliary substrate, thus acting as an anoxic sensitive element of the HIF system. Hypoxia inhibits PHD activity and increases the abundance and activity of HIF transcription complexes. |
| target | TargetValue PHD2 (Cell-free say) 21 nM |
| Target | Value |
| PHD2 (Cell-free assay) | 21 nM |
| in vivo research | to investigate the utility of IOX2 as in vivo functional Probes, IOX2 is tested to upregulate HIF signaling in a whole organism, that is, transgenic zebrafish ( Danio rerio ). Because the expression of the PHD3 encoding gene is regulated by HIF in humans and zebrafish, PHD3 levels are a readout of HIF activity. A zebrafish hypoxia reporter line is generated expressing GFP with the phd3 promoter elements. Transgenic wild-type embryos at 3 days postfertilization treated with compounds (10 μM) for 2 days displayed clear increase in phd3:EGFP expression in the liver, relative to controls. Significant increases in GFP levels are observed with IOX2. |
Last Update：2024-04-09 15:16:36
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