IOX4, PHD2 Inhibitor


Catalog No. size PriceQuantity
M60284-2S 2 mg solid $109
M60284-10S 10 mg solid $431

Description

Product Information
Molecular Weight: 328.33
Formula: C15H16N6O3
Purity: ≥98%
CAS#: 1154097-71-8
Solubility: DMSO up to 100 mM
Chemical Name: tert-butyl 6-(5-oxo-4-(1H-1,2,3-triazol-1-yl)-2,5-dihydro-1H-pyrazol-1-yl)nicotinate
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

 

Biological Activity:

IOX4 is a potent and selective PHD2 inhibitor with IC50 ~1.6 nM. It inhibits PHD2 via binding to the 2OG binding site, 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 ~5.6-11.7 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. IOX4 could be a useful tool compound for studies aimed at validating the upregulation of HIF for treatment of cerebral diseases including stroke.

How to Use:


In vitro: IOX4 was used at 10-50 µM final concentration in vitro and in cellular assays.
In vivo: IOX4 was dosed to mice by IP injection at 17.5-70 mg/kg. 


Reference:
  • 1. Chan MC, et al. Potent and Selective Triazole-Based Inhibitors of the Hypoxia-Inducible Factor Prolyl-Hydroxylases with Activity in the Murine Brain. (2015) PLoS One. 10(7):e0132004. 


Products are for research use only. Not for human use. 

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