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IOX2

HY-15468

(IOX 2; IOX-2)

IOX2

IOX2 Chemical Structure

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).

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Free sample   Apply now  
10 mM * 1 mL in DMSO $84 In-stock
5 mg $76 In-stock
10 mg $90 In-stock
50 mg $350 In-stock
100 mg Get quote
200 mg Get quote
Size Price Stock Quantity
Free sample   Apply now  
10 mM * 1 mL in DMSO €82 In-stock
5 mg €74 In-stock
10 mg €88 In-stock
50 mg €343 In-stock
100 mg Get quote
200 mg Get quote

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Product name: IOX2
Cat. No.: HY-15468

IOX2 Data Sheet

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    Purity: 99.58%

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Biological Activity of IOX2

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.

Protocol (Extracted from published papers and Only for reference)

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Chemical Information

M.Wt 352.34 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C19H16N2O5
CAS No 931398-72-0
Solvent & Solubility

DMSO 100 mg/ml

Preparing Stock Solutions

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

References on IOX2

Inhibitor Kit
  • 2-Methoxyestradiol

    2-methoxyestradiol (2ME2; NSC-659853) is a natural metabolite of estrogen that is known to inhibit HIF-1 alpha with an IC50 of 0.71 (plusmn) 0.11 (mu)M for the inhibition of BPAEC migration.

  • BAY 87-2243

    BAY 87-2243 is a highly potent and selective inhibitor of hypoxia-induced HIF-1 activation.

  • Chlorogenic acid

    Chlorogenic acid(NSC-407296; 3-O-Caffeoylquinic acid) is one of the most abundant polyphenols in the human diet, has been reported to inhibit cancer cell growth and a major anti-inflammatory constituent of lonicerae flos extract.

  • Daprodustat

    Daprodustat (GSK1278863) is a HIF-prolyl hydroxylase inhibitor.

  • DASA-58

    DASA-58 is a highly specific small molecule PKM2 activator. DASA-58 inhibits LPS-induced Hif-1a and IL-1b, as well as the expression of a range of other Hif-1a-dependent genes.

  • DMOG

    Dimethyloxallyl Glycine(DMOG) is a cell permeable, competitive inhibitor of HIF-PH(HIF-1(alpha) prolyl hydroxylase).

  • FG-2216

    FG-2216 is a potent HIF-prolyl hydroxylase inhibitor with IC50 of 3.9 uM for PDH2 enzyme; orally bioavailable and induced significant and reversible Epo induction in vivo.

  • FG-4592

    FG-4592 is an inhibitor of hypoxia inducible factor (HIF) prolyl hydroxylase currently in clinical development for the treatment of anemia.

  • HIF-2α-IN-1

    HIF-2(alpha)-IN-1 is a HIF-2(alpha) inhibitor has an IC50 of less than 500 nM in HIF-2(alpha) scintillation proximity assay.

  • JNJ-42041935

    JNJ-42041935 is a potent (pKi = 7.3-7.9), 2-oxoglutarate competitive, reversible, and selective inhibitor of PHD enzymes.

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