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IOX2(Glycine)HIF-1α prolyl hydroxylase-2 (PHD2) inhibitor

IOX2(Glycine)

Catalog No. A4189
Size Price Stock Qty
10mM (in 1mL DMSO) $85.00 In stock
Evaluation Sample $28.00 In stock
10mg $90.00 In stock
50mg $350.00 In stock

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Sample solution is provided at 25 µL, 10mM.

Quality Control

Quality Control & MSDS

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Chemical structure

IOX2

Biological Activity

Description IOX2 is a potent inhibitor of HIF-1α prolyl hydroxylase-2 (PHD2) with IC50 of 21 nM.
Targets PHD2          
IC50 21 nM          

Protocol

Kinase experiment [1]:

Alpha screen assay

All reagents were diluted in 50 mM HEPES, 0.1 % BSA, pH 7.5 supplemented with 0.01 % Tween20 and allowed to equilibrate to room temperature prior to addition to plates. Catalytic turnover assays were run in 10 μM volumes in low-volume 384-well plates at RT. The reaction consisted of enzyme (0.5 ~ 25 nM), biotinylated substrate peptide (30 ~ 1000 nM), Fe(II) (1 ~ 10 μM), Ascorbate (100 μM), 2OG (5 ~ 40 μM) and run at RT. EDTA was used to quench the reaction (5 μM) and AlphaScreen donor (Streptavidin-conjugated) and acceptor (ProteinA-conjugated) beads preincubated with peptide product antibodies were added (5 μM). Plates were foil-sealed to protect from light, incubated at room temperature for 60 mins and read on a PHERAstar FS plate reader using an AlphaScreen 680 excitation/570 emission filter set. The final bead concentration in 20 μM reaction was 20 μM/mL. IC50 values were calculated in Prism 5.

Cell experiment [1]:

Cell lines

RCC4 cells

Preparation method

The solubility of this compound in DMSO is > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20 °C for several months.

Reaction Conditions

50 μM

Applications

In RCC4 cells, IOX2 inhibited HIF-1α hydroxylation at 50 μM.

References:

[1]. Murray JK1, Balan C, Allgeier AM et al. Dipeptidyl-quinolone derivatives inhibit hypoxia inducible factor-1α prolyl hydroxylases-1, -2, and -3 with altered selectivity. J Comb Chem. 2010 Sep 13;12(5):676-86.

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Chemical Properties

Cas No. 931398-72-0 SDF Download SDF
Chemical Name 2-[(1-benzyl-4-hydroxy-2-oxoquinoline-3-carbonyl)amino]acetic acid
Canonical SMILES C1=CC=C(C=C1)CN2C3=CC=CC=C3C(=C(C2=O)C(=O)NCC(=O)O)O
Formula C19H16N2O5 M.Wt 352.34
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
General tips No
Shipping Condition No

Background

IOX2 is a novel and 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. [1, 2]

The hypoxia inducible factor (HIF) system is related to the signaling of low oxygen (hypoxia) in animals. The levels of HIF-α isoforms are controlled by an oxygen-dependent manner by the activity of the HIF prolyl-hydroxylases (PHD or EGLN enzymes), which are Fe(II) and 2-oxoglutarate (2OG) dependent oxygenases. IOX2 inhibits HIF-1α hydroxylation in RCC4 cells at 50 μM. [1, 2]

References:
Murray JK1, Balan C, Allgeier AM et al.  Dipeptidyl-quinolone derivatives inhibit hypoxia inducible factor-1α prolyl hydroxylases-1, -2, and -3 with altered selectivity. J Comb Chem. 2010 Sep 13;12(5):676-86. doi: 10.1021/cc100073a.
Chowdhury R1, Candela-Lena JI, Chan MC et al.  Selective small molecule probes for the hypoxia inducible factor (HIF) prolyl hydroxylases. ACS Chem Biol. 2013 Jul 19;8(7):1488-96. doi: 10.1021/cb400088q. Epub 2013 Jun 12.