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DPI (Diphenyleneiodonium chloride) NADPH-oxidase inhibitor

Name: DPI (Diphenyleneiodonium chloride)
Brand: Selleck Chemicals
SKU: S8639
Availability: InStock
Rating: 5 (48 reviews)

Cat.No.S8639

Diphenyleneiodonium chloride (DPI) is an inhibitor of NADPH oxidase and also a potent, irreversible, and time-, temperature-dependent iNOS/eNOS inhibitor. It also functions as a TRPA1 activator and selectively inhibits intracellular reactive oxygen species (ROS).

Chemical Structure

Molecular Weight: 314.55

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Quality Control

Batch: Purity: 99.69%

99.69

Related Targets	PD-1/PD-L1 CXCR STING AhR Immunology & Inflammation related CD markers Interleukins Anti-infection Antioxidant COX
Other NADPH-oxidase Inhibitors	Setanaxib (GKT137831) NAD+ (β-DPN) Apocynin GSK2795039 GLX351322 2-Acetylphenothiazine (ML171) VAS2870 gp91ds-tat Isuzinaxib (APX-115 free base)

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description	PMID
MC3T3-E1	Function assay	10 μM	30 min	block ROS generation and NOX expression	31049140
RAW264.7	Function assay	10 μM	4 days	DPI administration inhibited the effect of RANKL on osteoclast differentiation and reduced the number of TRAP-positive multinuclear cells	30942408
VSMC	Function assay	10 μM	6 h	diminished PDGF-BB-evoked VSMC dedifferentiation, proliferation and migration	29175753
HK-2	Function assay			inhibited ROS generation in the TZA-induced necroptosis	28894570
mouse neural precursor cells	Function assay			Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay	17417631
RAW264.7	Function assay		1 hr	Inhibition of LPS-stimulated ROS production in mouse RAW264.7 cells preincubated for 1 hr followed by LPS stimulation after 24 hrs by CMH2DCFDA probe-based fluorescence assay	28384544
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 13 mg/mL (41.32 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	3%DMSO 1 40%PEG300 2 2%Tween80 3 55%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.500mg/ml (1.59mM)	Taking the 1 mL working solution as an example, add 30 μL of clarified DMSO stock solution of 16.6666666666667 mg/ml to 400 μL of PEG300, mix evenly to clarify it; add 20 μL of Tween80 to the above system, mix evenly to clarify it; then continue to add 550 μL of ddH2O to make it clear. Volume up to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	314.55	Formula	C₁₂H₈I.Cl	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	4673-26-1	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	C1=CC=C2C(=C1)C3=CC=CC=C3[I+]2.[Cl-]

Mechanism of Action

Targets/IC₅₀/Ki	NADPH oxidase
In vitro	Diphenyleneiodonium chloride (DPI) inhibits the activity of NADPH oxidase, nitric oxide synthase, xanthine oxidase and NADPH cytochrome P450 oxidoreductase. Femtomolar concentrations of this compound exert potent anti-inflammatory and neuroprotective effects by inhibiting microglial activation through the inhibition of ERK-regulated PHOX activity. It has frequently been used to inhibit ROS production mediated by various flavoenzymes, including NAD(P)H oxidase, quinone oxidoreductase, cytochrome P450 reductase and nitric oxide synthase. NADPH, NADP+, and 2'5'-ADP blocks its inhibitory action. Treatment with DPI in ARPE-19 cells evoked a dose- and time-dependent growth inhibition, and also induced DNA fragmentation and protein content of the proapoptotic factor Bax. In addition, it signiﬁcantly induced the expression and phosphorylation of p53, which induces proapoptotic genes in response to DNA damage or irreparable cell cycle arrest. ROS have been implicated as a key factor in the activation of p53 by many chemotherapeutic drugs.
In vivo	Diphenyleneiodonium chloride (DPI), an NADPH oxidase inhibitor, inhibited the production of pro-inflammatory cytokines (TNF-α and IL-6), reduced macrophage infiltration and classical polarization, and induced ROS generation.
References	[1] https://pubmed.ncbi.nlm.nih.gov/21804230/ [2] https://pubmed.ncbi.nlm.nih.gov/9878531/ [3] https://pubmed.ncbi.nlm.nih.gov/1703974/ [4] https://pubmed.ncbi.nlm.nih.gov/17184774/ [5] https://pubmed.ncbi.nlm.nih.gov/32550901/

Applications

Methods	Biomarkers	Images	PMID
Western blot	Nox1 / MMP2 / MMP9		26760964

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT06061679	Not yet recruiting	COPD (Chronic Obstructive Pulmonary Disease) With Acute Lower Respiratory Infection	Fondazione Policlinico Universitario Agostino Gemelli IRCCS\|University of Florence UNIFI University of Florence Florence Italy Florence	November 2023	Not Applicable
NCT06111664	Recruiting	Mood Disorders	University Hospital Strasbourg France	May 1 2023	--
NCT05706129	Recruiting	Clear Cell Renal Cell Cancer (ccRCC)\|Pancreatic Ductal Adenocarcinoma (PDAC)\|Colorectal Cancer (CRC)	Debiopharm International SA	March 14 2023	Phase 1\|Phase 2
NCT05764681	Recruiting	Cerebral Palsy\|Chronic Post Surgical Pain	Chantel Burkitt\|National Institutes of Health (NIH)\|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD)\|University of Minnesota\|Nemours Children''s Hospital Delaware\|Gillette Children''s Specialty Healthcare	March 17 2023	--

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