IOX2(Glycine)

- Overview
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    Background
    
    IOX2 is a potent and selective inhibitor of HIF-1α prolyl hydroxylase-2 (PHD2) with an IC50 of 21 nM for PHD2/ELGN-1 in a cell-free assay, IOX2 has shown >100-fold selectivity over JMJD2A, JMJD2C, JMJD2E, JMJD3, or the 2OG oxygenase FIH [1].
    PHDs consist three isoforms, named PHD1, PHD2 and PHD3. PHDs are dioxygenases that utilize oxygen as co-substrate providing the molecular basis for the oxygen-sensing function of these enzymes. It has been reported that PHDs are strikingly sensitive to graded levels of hypoxia, mirroring the progressive increases in HIF-1α protein and DNA binding activity that are observed when cells are exposed to gradual hypoxia [2]. In RCC4 cells, IOX2 inhibited HIF-1α hydroxylation at 50 μM [1].
    
    [1] Murray J K, Balan C, Allgeier A M, et al. Dipeptidyl-quinolone derivatives inhibit hypoxia inducible factor-1α prolyl hydroxylases-1,-2, and-3 with altered selectivity[J]. Journal of combinatorial chemistry, 2010, 12(5): 676-686.
    [2] Berra E, Benizri E, Ginouvès A, et al. HIF prolyl‐hydroxylase 2 is the key oxygen sensor setting low steady‐state levels of HIF‐1α in normoxia[J]. The EMBO journal, 2003, 22(16): 4082-4090.
- Properties
  - Alternative Name
    
    2-[(1-benzyl-4-hydroxy-2-oxoquinoline-3-carbonyl)amino]acetic acid
    
    CAS Number
    
    931398-72-0
    
    Molecular Formula
    
    C19H16N2O5
    
    Molecular Weight
    
    352.34
    
    Appearance
    
    A solid
    
    Purity
    
    98.10%
    
    Solubility
    
    insoluble in EtOH; insoluble in H2O; ≥17.6 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Peng H, Purkerson JM, et al. "Acidosis induces antimicrobial peptide expression and resistance to uropathogenic E coli infection in kidney collecting duct cells via HIF-1α." Am J Physiol Renal Physiol. 2019 Dec 16. PMID:31841391
    2. Peng K, Chen WR, et al. "Dexmedetomidine post-treatment attenuates cardiac ischaemia/reperfusion injury by inhibiting apoptosis through HIF-1α signalling." J Cell Mol Med. 2020;24(1):850–861. PMID:31680420
    3. LUKE ERBER. "Functional Proteomics Analysis To Discover And Characterize Oxygen-Dependent Cellular Pathways." UNIVERSITY OF MINNESOTA. 2019.
    4. Zhou T, Erber L, et al. "Proteomic analysis reveals diverse proline hydroxylation-mediated oxygen-sensing cellular pathways in cancer cells." Oncotarget. 2016 Nov 29;7(48):79154-79169. PMID:27764789

IOX2(Glycine)

Background

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