931398-72-0 Usage
Description
IOX2 is a potent inhibitor of HIF-1α prolyl hydroxylase-2 (PHD2) with an IC50 of 21 nM. It is a small molecule compound that can modulate cellular responses to hypoxia by inhibiting the activity of PHD2, a key enzyme involved in the regulation of hypoxia-inducible factor-1α (HIF-1α).
Uses
Used in Pharmaceutical Industry:
IOX2 is used as a PHD inhibitor for inducing pseudo-hypoxia in cells. This application is valuable in studying the effects of hypoxia on cellular processes and developing potential therapeutic agents targeting hypoxia-related diseases.
Used in Research Applications:
IOX2 is used as a research tool to investigate the role of HIF-1α and PHD2 in various cellular and molecular pathways. By inhibiting PHD2, IOX2 can help researchers gain insights into the mechanisms underlying hypoxia-induced gene expression and cellular adaptation to low oxygen conditions.
Biological Activity
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].
Biochem/physiol Actions
IOX2 is selective and potent inhibitor of prolyl hydroxylases (PHD). Stabilization of HIF-1R through inhibition of PHD has been examined as a potential treatment for ischemic diseases including anemia, myocardial infarction, and stroke. IOX2 is a selective inhibitor of the hypoxia inducible factor (HIF) prolyl-hydroxylases (PHD) that exhibits up-regulation of HIF1a in zebrafish. For full characterization details, please visit the IOX2 probe summary on the Structural Genomics Consortium (SGC) website.To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
references
[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.
Check Digit Verification of cas no
The CAS Registry Mumber 931398-72-0 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 9,3,1,3,9 and 8 respectively; the second part has 2 digits, 7 and 2 respectively.
Calculate Digit Verification of CAS Registry Number 931398-72:
(8*9)+(7*3)+(6*1)+(5*3)+(4*9)+(3*8)+(2*7)+(1*2)=190
190 % 10 = 0
So 931398-72-0 is a valid CAS Registry Number.
InChI:InChI=1S/C19H16N2O5/c22-15(23)10-20-18(25)16-17(24)13-8-4-5-9-14(13)21(19(16)26)11-12-6-2-1-3-7-12/h1-9,24H,10-11H2,(H,20,25)(H,22,23)
931398-72-0Relevant articles and documents
PROLYL HYDROXYLASE ANTAGONISTS
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Page/Page column 19, (2010/11/26)
This invention relates to certain 2-[(quinolin-3-yl)carbonyl]aminoacetic acid derivatives of formula (I), where the various groups are defined herein, and which are useful in treating anemia.
