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IOX2 is a potent inhibitor of HIF-1α prolyl hydroxylase-2 (PHD2) with IC50 of 21 nM, >100-fold selectivity over JMJD2A, JMJD2C, JMJD2E, JMJD3, or the 2OG oxygenase FIH. IOX2 efficiently promotes HIF-1α stability, nuclear translocation, and target gene expression in keratinocytes and fibroblasts. In addition, IOX2 significantly upregulates biosynthesis and transcription of VEGF-A and BNIP3 in sulfur mustard (SM)-exposed NHEK and NHDF grown under hypoxia.
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Source | Sci Rep (2017). Figure 5. IOX2 |
| Method | RT-PCR | |
| Cell Lines | Primary articular chondrocytes | |
| Concentrations | 20 μM | |
| Incubation Time | 72 hours | |
| Results | We found that expression of proliferation markers, p57 and cyclin D1, were both reduced by 28% |
| Molecular Weight | 352.34 |
| Formula | C19H16N2O5 |
| CAS Number | 931398-72-0 |
| Solubility (25°C) | DMSO 10 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related HIF Products |
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| FG-4592 (Roxadustat)
FG-4592 (Roxadustat; ASP1517) is a novel Hypoxia Inducible Factor Prolyl Hydroxylase inhibitor. |
| 2-Methoxyestradiol
2-methoxyestradiol (2-ME2), an endogenous metabolite of 17β -estradiol (E2) with oral activity, is an apoptosis inducer and angiogenesis inhibitor with effective antitumor activity. Methoxyestradiol can also destabilize microtubules. Methoxyestradiol is a potent inhibitor of superoxide dismutase (SOD) and reactive oxygen species (ROS) that can induce autophagy in transformed cell line HEK293, cancer cell line U87 and HeLa. |
| DMOG
DMOG (Dimethyloxaloyl glycine) is an antagonist of α-ketoglutarate cofactor and a cell permeable and competitive inhibitor of HIF-PH, which results in HIF-1α stabilisation and accmulation in vitro and in vivo. DMOG acts as a pro-angiogenic agent and plays a protective role in experimental model of colitis and diarrhoea via HIF-1 related signal. DMOG induces cell autophagy. |
| Hydralazine hydrochloride
Hydralazine hydrochloride is a hydrochloride salt of hydralazine (Apresoline) that is a direct-acting smooth muscle relaxant with an IC50 of 1.9 mM. |
| Paeoniflorin
Paeoniflorin is a glycoside isolated from the root of Paeonia lactiflora. Paeoniflorin has been used as an anticonvulsant and has hypoglycemic effect. |
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