research use only

DPI (Diphenyleneiodonium chloride) NADPH-oxidase inhibitor

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).
DPI (Diphenyleneiodonium chloride) NADPH-oxidase inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 314.55

Quality Control

Cell Culture, Treatment & Working Concentration

Cell Lines Assay Type Concentration Incubation Time Formulation 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

Chemical Information, Storage & Stability

Molecular Weight 314.55 Formula

C12H8I.Cl

Storage (From the date of receipt)
CAS No. 4673-26-1 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles C1=CC=C2C(=C1)C3=CC=CC=C3[I+]2.[Cl-]

Solubility

In vitro
Batch:

DMSO : 13 mg/mL ( (41.32 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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

mg/kg g μL

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.

Mechanism of Action

Targets/IC50/Ki
NADPH oxidase [1]
In vitro

Diphenyleneiodonium chloride (DPI) inhibits the activity of NADPH oxidase, nitric oxide synthase, xanthine oxidase and NADPH cytochrome P450 oxidoreductase[4].

Femtomolar concentrations of this compound exert potent anti-inflammatory and neuroprotective effects by inhibiting microglial activation through the inhibition of ERK-regulated PHOX activity[1].

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[2].

NADPH, NADP+, and 2'5'-ADP blocks its inhibitory action[3].

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[4].

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
  • https://pubmed.ncbi.nlm.nih.gov/17184774/
  • https://pubmed.ncbi.nlm.nih.gov/32550901/

Applications

Methods Biomarkers Images PMID
Western blot Nox1 / MMP2 / MMP9 S8639-WB1 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 --

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.