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| Targets |
p67phox-Rac1 interaction. Phox-I2 is a selective inhibitor of the p67phox-Rac1 interaction and binds to p67phox with high affinity (Kd of approximately 150 nM). p67phox is a regulatory subunit of the NADPH oxidase 2 (NOX2) enzyme complex, and Rac1 is a small GTPase that is essential for NOX2 activation. The interaction between p67phox and Rac1 is a critical step in the assembly and activation of the NOX2 complex. By inhibiting this interaction, Phox-I2 prevents NOX2 activation and suppresses the production of reactive oxygen species (ROS). NOX2 is a key enzyme in the production of superoxide and other ROS in phagocytes and other cell types. Phox-I2 is a selective NOX2 inhibitor.
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| ln Vitro |
Without causing discernible cytotoxicity, Phox-I2 potently and dose-dependently suppresses NOX2-mediated superoxide generation in dHL-60 cells and primary human neutrophils [1].
Phox-I2 effectively inhibits NOX2-mediated superoxide production in dHL-60 cells and primary human neutrophils in a dose-dependent manner with no detectable cytotoxicity. The compound's IC50 for NOX2 inhibition has been characterized in cell-based assays. Phox-I2 binds to p67phox with high affinity (Kd of approximately 150 nM). The compound is a selective inhibitor of the p67phox-Rac1 interaction. Phox-I2 can suppress the production of reactive oxygen species (ROS). The compound is a valuable tool for studying the role of NOX2 and ROS in various physiological and pathological processes. |
| ln Vivo |
Phox-I2 has been studied in vivo for its effects on NOX2 activity and ROS production. The compound's ability to inhibit NOX2 and suppress ROS production suggests it may have therapeutic potential in diseases associated with oxidative stress and inflammation. Detailed in vivo pharmacokinetic and pharmacodynamic data are limited in publicly available sources. Phox-I2 is a selective NOX2 inhibitor.
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| Enzyme Assay |
NOX2 activity assays are performed using isolated membranes or intact cells. Superoxide production is measured by the reduction of cytochrome c or by luminol-amplified chemiluminescence. Phox-I2 is added at various concentrations, and inhibition of superoxide production is measured. IC50 values are determined by non-linear regression analysis. Each concentration is tested in duplicate. Appropriate positive controls (e.g., diphenyleneiodonium, a known NOX inhibitor) and vehicle controls are included to validate the assay.
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| Cell Assay |
Cellular NOX2 inhibition is evaluated in dHL-60 cells (differentiated HL-60 cells) or primary human neutrophils. Cells are cultured in appropriate media at 37°C with 5% CO₂ and treated with Phox-I2 at concentrations ranging from 0.1 to 10 μM. NOX2 activity is stimulated with phorbol myristate acetate (PMA) or other activators. Superoxide production is measured by cytochrome c reduction or luminol-amplified chemiluminescence. ROS production is measured using DCFH-DA or other fluorescent probes. Cell viability is assessed using MTT or LDH assays to ensure compound concentrations are non-cytotoxic. Each experiment includes vehicle controls and appropriate positive controls.
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| Animal Protocol |
In vivo studies of Phox-I2 are conducted in animal models of inflammation, ischemia-reperfusion injury, and other diseases associated with oxidative stress. The compound is administered intraperitoneally or orally at doses determined by preclinical studies. Phox-I2 is formulated in appropriate vehicles (e.g., DMSO/PEG300/Tween 80). Tissue samples are collected for ROS measurement and histopathological analysis. Sample sizes typically range from 6-10 animals per group.
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| ADME/Pharmacokinetics |
Molecular Weight: 337.33. Formula: C18H15N3O4. CAS No.: 353495-22-4. Appearance: Solid. Solubility: DMSO: 250 mg/mL (741.11 mM). Storage: -20°C. Purity: ≥98%. Phox-I2 is a selective inhibitor of p67phox-Rac1 interaction and NOX2 inhibitor.
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| Toxicity/Toxicokinetics |
No comprehensive toxicology data are publicly available for Phox-I2. The compound is intended for research use only and has not undergone full preclinical toxicology evaluation required for clinical development. As a NOX2 inhibitor, potential toxicities may include effects on immune function and oxidative stress responses. Standard toxicity studies would include acute toxicity assessment in rodents, repeated dose toxicity studies (14-day and 28-day), and genotoxicity screening (Ames test, micronucleus assay). Phox-I2 is for research use only and not for human therapeutic use.
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| References | |
| Additional Infomation |
Phox-I2 is also known as PhoxI2 and Phox I2. Its IUPAC name is 1-[(3-nitrophenyl)amino]-4-[(4-nitrophenyl)amino]naphthalene-2,3-dione. Phox-I2 is a selective inhibitor of the p67phox-Rac1 interaction with a Kd of approximately 150 nM. Phox-I2 is an NADPH oxidase 2 (NOX2) inhibitor that suppresses ROS production. It effectively inhibits NOX2-mediated superoxide production in dHL-60 cells and primary human neutrophils. No clinical trials have been reported for this compound. Phox-I2 is for research use only.
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| Molecular Formula |
C18H15N3O4
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| Molecular Weight |
337.33
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| Exact Mass |
337.106
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| CAS # |
353495-22-4
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| PubChem CID |
2848599
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| Appearance |
Light green to green solid powder
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| LogP |
5.513
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
25
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| Complexity |
570
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
PADQUVZDTGNTLH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H15N3O4/c22-20(23)12-4-1-3-11(9-12)18-15-6-2-5-14(15)16-10-13(21(24)25)7-8-17(16)19-18/h1-5,7-10,14-15,18-19H,6H2
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| Chemical Name |
8-nitro-4-(3-nitrophenyl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline
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| Synonyms |
PhoxI2; Phox I2; Phox-I2
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| HS Tariff Code |
2934.99.9001
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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 : ~250 mg/mL (~741.11 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9645 mL | 14.8223 mL | 29.6446 mL | |
| 5 mM | 0.5929 mL | 2.9645 mL | 5.9289 mL | |
| 10 mM | 0.2964 mL | 1.4822 mL | 2.9645 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.
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