IOX2 931398-72-0

.cp_wz table {border-top: 1px solid #ccc;border-left:1px solid #ccc; } .cp_wz table td{border-right: 1px solid #ccc; border-bottom: 1px solid #ccc; padding: 5px 0px 0px 5px;} .cp_wz table th {border-right: 1px solid #ccc;border-bottom: 1px solid #ccc; padding: 5px 0px 0px 5px;}


Molecular Weight:

352.34 IOX2 is a Potent Inhibitor of HIF-1α prolyl hydroxylase-2 (PHD2) with IC50 of 21 nM, >100-fold selectivity over JMJD2A, JMJD2C, JMJD2E, JMJD3, or the 2OG oxygenase FIH.


Biological Activity


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 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.






Alpha Screen Assay


All reagents are 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 are run in 10 μM
volumes in low-volume 384-well plates at RT. The reaction consists of
enzyme (0.5-25nM), biotinylated substrate peptide (30-1000 nM), Fe(II)
(1-10 μM), Ascorbate (100 μM), 2OG (5-40 μM) and run at RT. EDTA is used
to quench the reaction (5 μM) and AlphaScreen donor
(Streptavidin-conjugated) and acceptor (ProteinA-conjugated) beads
preincubated with peptide product antibodies are added (5 μM).


Plates
are foil-sealed to protect from light, incubated at room temperature for
60 minutes 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 is 20 μM/mL. IC50 values are calculated in Prism 5 after
normalization against corresponding DMSO c

Contact us if you need more details on 931398-72-0. We are ready to answer your questions on packaging, logistics, certification or any other aspects about IOX2 931398-72-0、931398-72-0 IOX2. If these products fail to match your need, please contact us and we would like to provide relevant information.

Product Categories : Epigenetics > HIF Inhibitor