| Field | Specification |
|---|---|
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C19H16N2O5 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
IOX2 is a chemical probe that acts as a specific inhibitor of prolyl hydroxylase-2 (PHD2), with an IC50 of 22 nM. It regulates platelet function and arterial thrombosis by upregulating HIF-1α expression and suppressing ROS production, and it can be used to study thrombotic diseases[1][2]. It is supplied as a white to off-white solid (C19H16N2O5, MW 352.34) at 98.02% purity.
Physical & Chemical Properties
| CAS Number | 931398-72-0 |
|---|---|
| Molecular Formula | C19H16N2O5 |
| Molecular Weight | 352.34 g/mol |
| Purity | 98.02% |
| Appearance | Solid |
| Color | White to off-white |
| SMILES | O=C(O)CNC(C1=C(O)C2=C(N(CC3=CC=CC=C3)C1=O)C=CC=C2)=O |
| Signaling Pathway | Metabolic Enzyme/Protease |
| Solubility | In Vitro: DMSO: 25 mg/mL (70.95 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 2 years; -20°C, 1 year. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target
IC50: 22 nM (PHD2)[2]
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 25 mg/mL (70.95 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 2 years) or -20°C (up to 1 year); avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 2.5 mg/mL (7.10 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Data provided by the manufacturer.
In Vitro
IOX2 (0, 10, 25, and 50 μM) dose-dependently inhibits platelet aggregation and ATP release induced by collagen-related peptide (CRP; 0.25 μg/mL) or thrombin (0.03 U/mL). IOX2 does not, however, affect P-selectin expression or the surface levels of glycoprotein (GP)Ibα, GPVI, or αIIbβ3[1]. IOX2 also blocks platelet spreading on fibrinogen or collagen, as well as clot retraction[1]. In Normal human epidermal keratinocytes (NHEK) and Normal human dermal fibroblasts (NHDF) grown under normoxia and hypoxia conditions, IOX2 (50 μM; 24 h) raises the transcription levels of VEGF-A and BNIP3[2].
In Vivo
In mice, IOX2 (10 mg/kg; i.p.; single dose) impaired platelet hemostatic function in vivo as well as arterial thrombus formation[1].
| Animal Model | Mouse[1] |
|---|---|
| Dosage | 10 mg/kg |
| Administration | Intraperitoneal injection |
| Result | Upregulated HIF-1α in platelets, decreased 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. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. Nat Commun 2026 Feb 12;17(1):1214. PMID: 41680175
Dual functions of microRNA-17 in maintaining cartilage homeostasis and protection against osteoarthritis. Nat Commun 2022 May 4;13(1):2447. PMID: 35508470
Ginsenoside CK targets PHD2 to prevent platelet adhesion and enhance blood circulation by modifying the three-dimensional arrangement of collagen. Acta Pharm Sin B 2025 Mar;15(3):1497-1513. PMID: 40370536
SIRT5-mediated desuccinylation of PPA2 enhances HIF-1alpha-dependent adaptation to hypoxic stress and colorectal cancer metastasis. EMBO J 2025 May;44(9):2514-2540. PMID: 40164945
Metabolic disruption exacerbates intestinal damage during sleep deprivation by abolishing HIF1α-mediated repair. Cell Rep 2024 Nov 10;43(11):114915. PMID: 39527478
Inhibition of Hypoxia-Inducible Factor Prolyl-Hydroxylase Modulates Platelet Function. Thromb Haemost 2022 Oct;122(10):1693-1705. PMID: 35477177
Deciphering glutamine metabolic reprogramming: a novel therapeutic target ALDH18A1 in triple-negative breast cancer. Sci Rep 2026 Jun 20. PMID: 42323345
EGLN1 inhibition reverses angiogenesis impairment in hyperglycemia by activating autophagy. Sci Rep 2025 Oct 14;15(1):35804. PMID: 41087486
Hypoxia-induced HIF1α activation regulates small extracellular vesicle release in human embryonic kidney cells. Sci Rep 2022 Jan 27;12(1):1443. PMID: 35087095
Hypoxia-Inducible Factor-1 α in Macrophages, but Not in Neutrophils, Is Important for Host Defense during Klebsiella pneumoniae-Induced Pneumosepsis. Mediators Inflamm 2021 Aug 5:2021:9958281. PMID: 34393650