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Purity: ≥98%
IOX2 is a novel and potent inhibitor of hypoxia-inducible factor (HIF-1α) prolyl hydroxylase-2 (PHD2) with considerable medical uses. It inhibits PHD2 with an IC50 of 21 nM in a cell-free assay,and displays >100-fold selectivity over JMJD2A, JMJD2C, JMJD2E, JMJD3, or the 2OG oxygenase FIH.
| ln Vitro |
Thrombin (0.03 U/mL) or collagen-related peptide (CRP; 0.25 μg/mL)-induced platelet aggregation and ATP release were dose-dependently inhibited by IOX2 (0, 10, 25, and 50 μM). IOX2 does not, however, alter the expression of P-selectin or the surface concentrations of GPVI, αIIbβ3, or glycoprotein (GP)Ibα[1]. In addition to preventing clot retraction, IOX2 also prevents platelet spreading on collagen or fibrinogen [1]. Normal human dermal fibroblasts (NHDF) and epidermal keratinocytes (NHEK) grown in normoxic and hypoxic conditions exhibit increased transcript levels of VEGF-A and BNIP3 in response to IOX2 (50 μM; 24 h) [2].
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| ln Vivo |
In mice, IOX2 (10 mg/kg; i.p.; single dose) reduces platelet hemostatic activity and causes arterial thrombosis [1].
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| Animal Protocol |
Animal/Disease Models: Mouse[1]
Doses: 10 mg/kg Route of Administration: intraperitoneal (ip)injection Experimental Results: Upregulated HIF-1α in platelets, diminished ROS generation, and downregulated NOX1 expression. Increased the phosphorylation level of VASP (Ser157/239), and inhibited the Phosphorylation of p38 (Thr180/Tyr182), ERK1/2 (Thr202/Tyr204), AKT (Thr308/Ser473), and PKCδ (Thr505) in CRP- or thrombin-stimulated platelets. |
| References |
[1]. Gu W, et al. Inhibition of Hypoxia-Inducible Factor Prolyl-Hydroxylase Modulates Platelet Function. Thromb Haemost. 2022 Oct;122(10):1693-1705.
[2]. Deppe J, et al. Impairment of hypoxia-induced HIF-1α signaling in keratinocytes and fibroblasts by sulfur mustard is counteracted by a selective PHD-2 inhibitor. Arch Toxicol. 2016 May;90(5):1141-50. |
| Molecular Formula |
C19H16N2O5
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|---|---|
| Molecular Weight |
352.3407
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| CAS # |
931398-72-0
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| Related CAS # |
IOX2 sodium;2377239-85-3
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| SMILES |
O([H])C1=C(C(N([H])C([H])([H])C(=O)O[H])=O)C(N(C([H])([H])C2C([H])=C([H])C([H])=C([H])C=2[H])C2=C([H])C([H])=C([H])C([H])=C21)=O
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| Synonyms |
IOX-2; IOX2; IOX 2
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 7 mg/mL (19.9 mM)
Water:<1 mg/mL
Ethanol:<1 mg/mL
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| Solubility (In Vivo) |
Chemical Name:N-[[1,2-Dihydro-4-hydroxy-2-oxo-1-(phenylmethyl)-3-quinolinyl]carbonyl]glycineInChi Key:CAOSCCRYLYQBES-UHFFFAOYSA-NInChi Code: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)SMILES Code:O=C(O)CNC(C1=C(O)C2=C(N(CC3=CC=CC=C3)C1=O)C=CC=C2)=O (Please use freshly prepared in vivo formulations for optimal results.)
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| 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
J Biol Chem. 2011 Apr 15;286(15):13041-51. |
Levels of HIF asparaginyl hydroxylation in hypoxic cells and in rat and human tissues. J Biol Chem. 2011 Apr 15;286(15):13041-51. |
Differential inhibition of HIF prolyl and asparaginyl hydroxylation by HIF hydroxylase inhibitors. J Biol Chem. 2011 Apr 15;286(15):13041-51. |
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