IOX2

Catalog No.S2919 Synonyms: JICL38

IOX2 Chemical Structure

Molecular Weight(MW): 352.34

IOX2 is a potent inhibitor of HIF-1α prolyl hydroxylase-2 (PHD2) with IC50 of 21 nM in a cell-free assay, >100-fold selectivity over JMJD2A, JMJD2C, JMJD2E, JMJD3, or the 2OG oxygenase FIH.

Size Price Stock Quantity  
In DMSO USD 190 In stock
USD 147 In stock
USD 570 In stock
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2 Customer Reviews

  • NHEK and NHDF are cultivated under normoxic (N) and hypoxic (H) conditions in the presence of IOX2 (50 μM), or vehicle control (DMSO). b HIF-1α levels are analyzed in cell extracts of NHEK (4 h) and NHDF (24 h) by immunoblotting with cellular β-actin as loading control. c Subcellular localization of HIF-1α is examined by immunoblotting analysis of HIF-1α in nuclear (Nu) and cytoplasmic (Cy) fractions with β-tubulin as cytosolic loading control.

    Arch Toxicol, 2016, 90(5):1141-50. IOX2 purchased from Selleck.

    Immunocytochemistry analysis of HIF-1α in NHEK and NHDF after incubation with a PHD-2 inhibitor, IOX2 (50 μM), or vehicle control (DMSO) for 4 h. Scale bars 100 μm.

    Arch Toxicol, 2015, 10.1007/s00204-015-1549-y . IOX2 purchased from Selleck.

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Biological Activity

Description IOX2 is a potent inhibitor of HIF-1α prolyl hydroxylase-2 (PHD2) with IC50 of 21 nM in a cell-free assay, >100-fold selectivity over JMJD2A, JMJD2C, JMJD2E, JMJD3, or the 2OG oxygenase FIH.
Targets
PHD2 [1]
(Cell-free assay)
21 nM
In vitro

IOX2 potently inhibits PHD2 (IC50 of 21 nM) with over 100-fold selectivity compared to inhibition of JMJD2A, JMJD2C, JMJD2E, JMJD3, or the 2OG oxygenase FIH (IC50s <100 μM). IOX2 is active in cells, inhibiting HIF-1α hydroxylation in RCC4 cells at 50 μM. [1] Hypoxia Inducible Factor (HIF) is regulated by the hydroxylation of prolyl residues in oxygen-dependent degradation domains in the HIF-1α subunit, which mark it for degradation by the proteosome. 1,2 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 cosubstrate, thus acting as the hypoxia-sensing component of the HIF system. The activity of PHD is suppressed by hypoxia, increasing both the abundance and activity of the HIF transcriptional complex. [2]

Protocol

Solubility (25°C)

In vitro DMSO 7 mg/mL (19.86 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents individually and in order:
5% DMSO+30% PEG 300+ddH2O
2mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 352.34
Formula

C19H16N2O5

CAS No. 931398-72-0
Storage powder
in solvent
Synonyms JICL38

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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HIF Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID