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Products are for research use only. Not for human use. We do not sell to patients.
(IOX 2; IOX-2)
IOX2 Chemical Structure
|Product name: IOX2|
|Cat. No.: HY-15468|
IOX2 is a selective inhibitor of the Hypoxia Inducible Factor (HIF) Prolyl-Hydroxylases (PHD); active in cells with IC50 value of 21 nM for PHD2/ELGN-1 and no inhibition at FIH (20uM).
IC50 value: 21 nM
Target: HIF Prolyl-Hydroxylases
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. 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. IOX2 potently inhibits PHD2 (IC50 value 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.
|M.Wt||352.34||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
10 mM in DMSO
|1 mg||5 mg||10 mg|
|1 mM||2.8382 mL||14.1908 mL||28.3817 mL|
|5 mM||0.5676 mL||2.8382 mL||5.6763 mL|
|10 mM||0.2838 mL||1.4191 mL||2.8382 mL|
. Flashman E, et al. Kinetic rationale for selectivity toward N- and C-terminal oxygen-dependent degradation domain substrates mediated by a loop region of hypoxia-inducible factor prolyl hydroxylases. J Biol Chem. 2008 Feb 15;283(7):3808-15.
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