| Cat.No.: | BSM-0394 |
| Product Name: | IOX4 |
| CAS No.: | 1154097-71-8 |
| Figure: |
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| Product Overview: | A selective, bioavailable inhibitor of PHD2 |
| Description: | Hypoxia-inducible factors (HIFs) are regulated by the hydroxylation of prolyl residues in oxygen-dependent degradation domains, which leads to degradation by the proteasome. HIF prolyl hydroxylation is catalyzed by prolyl hydroxylase domain enzymes (PHD1, 2, and 3), members of the Fe(II) and 2-oxoglutarate (2OG) oxygenase family. They require dioxygen as a co-substrate, thus acting as the hypoxia-sensing component of the HIF system. IOX4 is a potent inhibitor of PHD2 (IC50 = 1.6 nM). It displays >1,000-fold selectivity for PHD2 over other 2OG-dependent dioxygenases, including JMJD isoforms, FBXL11, JARID1C, BBOX1, FIH, and FTO. IOX4 is active in vivo, inhibiting prolyl hydroxylation and increasing HIF-1α levels in cells (IC50 values range from 5.6 to 11.7 µM) and inducing HIF-1α and HIF-2α expression in mice. The induction of HIF expression in mice occurs in the brain as well as in the liver, kidney, and heart, indicating that IOX4 penetrates the blood-brain barrier. |
| Appearance: | A crystalline solid |
| Molecular Weight: | 328.3 |
| Purity: | ≥98% |
| Storage: | -20°C |
| Targets: | PHD2 |
| Molecular Formula: | C15H16N6O3 |
| Chemical Name: | 1,1-dimethylethyl ester 6-[2,5-dihydro-5-oxo-4-(1H-1,2,3-triazol-1-yl)-1H-pyrazol-1-yl]-3-pyridinecarboxylic acid |
| Warning: | For Research Use Only! Not For Use in Humans. |
| Product Types | ||
| ◆ Antibodies | ||
| EAb-0056 | PHF8 Polyclonal Antibody | Inquiry |
| EAb-0058 | PHC2 Polyclonal Antibody | Inquiry |
| ◆ Bioactive Small Molecules | ||
| BSM-0114 | DMOG | Inquiry |
| ◆ Cell Lines | ||
| CL-0115 | Human PHF6 Knockout Cell Line 1bp deletion | Inquiry |
| CL-0116 | Human PHIP Knockout Cell Line 2bp deletion | Inquiry |
| Related Gene / Proteins | |||
| PHB | PHC1 | PHC2 | PHD |
| PHD1 | PHD2 | PHD3 | PHF1 |
| PHF10 | PHF13 | PHF17 | PHF2 |
| PHF20 | PHF20B | PHF21A | PHF21B |
| PHF6 | PHF8 | PHIP | PHPT1 |
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