DPQ (Synonyms: PARP Inhibitor III) |
Catalog No.GC15294
One-Click Copy Product Info
|
DPQ is a potent, blood-brain barrier-permeable poly(ADP-ribose) polymerase-1 (PARP-1) selective inhibitor used to study DNA damage repair and related cellular processes.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 129075-73-6
Sample solution is provided at 25 µL, 10mM.
DPQ is a potent, blood-brain barrier-permeable poly(ADP-ribose) polymerase-1 (PARP-1) selective inhibitor used to study DNA damage repair and related cellular processes[1-2]. DPQ can be applied to investigate inflammatory responses and cell death mechanisms in acute lung injury, myocardial ischemia-reperfusion injury, and neurodegenerative diseases, demonstrating neuroprotective and cardioprotective effects[3-4].
In vitro, pretreatment of non-small cell lung cancer cells (A549 and H1299) with DPQ (1μM) for 4 hours, followed by carbon ion irradiation (0.5–2Gy) for 24 hours, significantly inhibited cell migration, wound healing capacity, and the activity and expression of matrix metalloproteinases (MMP-2 and MMP-9)[5]. Pretreatment of HeLa cells with DPQ (20–150μM) for 1 hour, followed by stimulation with PMA (50nM) for 3 hours, significantly suppressed the upregulation of histamine H1 receptor (H1R) gene expression and reduced H1R promoter activity[6].
In vivo, pretreatment of C57BL/6 mice with DPQ (15mg/kg) 24 hours before renal ischemia for 45 minutes/reperfusion for 6 hours reduced ischemia-reperfusion-related pathological damage, such as acute tubular necrosis (ATN), tubular cell vacuolization, and brush border loss, by inhibiting PARP-1 overactivation, while also ameliorating tubular epithelial cell shedding and cast formation[7]. Pretreatment of C57BL/6 mice with LPS (7.5mg/kg) for 30 minutes, followed by intraperitoneal injection of DPQ (10μg/kg) for 6 hours, significantly inhibited neutrophil infiltration and myeloperoxidase (MPO) activity in lung tissue, while reducing the mRNA expression levels of pro-inflammatory factors such as TNF-α, IL-1β, and IL-6[8].
References:
[1] Meli E, Pangallo M, Picca R, et al. Differential role of poly(ADP-ribose) polymerase-1in apoptotic and necrotic neuronal death induced by mild or intense NMDA exposure in vitro. Mol Cell Neurosci. 2004 Jan;25(1):172-80.
[2] Wang J, Hao L, Wang Y, et al. Inhibition of poly (ADP-ribose) polymerase and inducible nitric oxide synthase protects against ischemic myocardial damage by reduction of apoptosis. Mol Med Rep. 2015 Mar;11(3):1768-76.
[3] Czapski GA, Cakala M, Kopczuk D, et al. Effect of poly(ADP-ribose) polymerase inhibitors on oxidative stress evoked hydroxyl radical level and macromolecules oxidation in cell free system of rat brain cortex. Neurosci Lett. 2004 Feb 6;356(1):45-8.
[4] Suh SW, Aoyama K, Alano CC, et al. Zinc inhibits astrocyte glutamate uptake by activation of poly(ADP-ribose) polymerase-1. Mol Med. 2007 Jul-Aug;13(7-8):344-9.
[5] Chowdhury P, Dey P, Ghosh S, et al. Reduction of metastatic potential by inhibiting EGFR/Akt/p38/ERK signaling pathway and epithelial-mesenchymal transition after carbon ion exposure is potentiated by PARP-1 inhibition in non-small-cell lung cancer. BMC Cancer. 2019 Aug 22;19(1):829.
[6] Mizuguchi H, Terao T, Kitai M, et al. Involvement of protein kinase Cdelta/extracellular signal-regulated kinase/poly(ADP-ribose) polymerase-1 (PARP-1) signaling pathway in histamine-induced up-regulation of histamine H1 receptor gene expression in HeLa cells. J Biol Chem. 2011 Sep 2;286(35):30542-30551.
[7] del Moral RM, Gómez-Morales M, Hernández-Cortés P, et al. PARP inhibition attenuates histopathological lesion in ischemia/reperfusion renal mouse model after cold prolonged ischemia. ScientificWorldJournal. 2013 Nov 11;2013:486574.
[8] Wang G, Huang X, Li Y, et al. PARP-1 inhibitor, DPQ, attenuates LPS-induced acute lung injury through inhibiting NF-κB-mediated inflammatory response. PLoS One. 2013 Nov 21;8(11):e79757.
| Cell experiment [1]: | |
Cell lines | A549 and H1299 (human non-small cell lung cancer cells), HeLa (human cervical cancer cells), MCF7 (human breast adenocarcinoma cells) |
Preparation Method | Cells were maintained in DMEM supplemented with 10% fetal bovine serum (FBS) at 37°C, 5% CO₂. Cells were treated with DPQ (1μM) 4 hours prior to carbon ion (¹²C) irradiation and cultured in the presence of DPQ post-irradiation. |
Reaction Conditions | 1μM; 4h pre-treatment followed by ¹²C irradiation (0.5–2Gy) |
Applications | DPQ significantly suppressed cell migration and wound healing in A549 and H1299 cells by inhibiting phosphorylation of EGFR, Akt, p38, and ERK, leading to inactivation of NF-κB. DPQ reduced MMP-2 and MMP-9 expression. DPQ also inhibited epithelial-mesenchymal transition (EMT) by downregulating N-cadherin, vimentin, and anillin while upregulating claudin-1 and claudin-2. |
| Animal experiment [2]: | |
Animal models | C57BL/6 mice (8–10 weeks old, male) |
Preparation Method | Mice were intraperitoneally injected with LPS (7.5mg/kg) to induce acute lung injury. DPQ (1 or 10μg/kg) was administered intraperitoneally 30 minutes after LPS challenge. Mice were sacrificed 6 hours post-LPS exposure for lung tissue analysis. |
Dosage form | 10μg/kg; i.p.; Single injection. |
Applications | DPQ treatment significantly attenuated LPS-induced acute lung injury by reducing neutrophil infiltration and inhibiting vascular permeability. DPQ suppressed mRNA expression of pro-inflammatory mediators (TNF-α, IL-1β, IL-6, MIP-2, iNOS, and CXCL-1) in lung tissues and decreased apoptotic cell death. |
References: | |
| Cas No. | 129075-73-6 | SDF | |
| Synonyms | PARP Inhibitor III | ||
| Chemical Name | 5-(4-(piperidin-1-yl)butoxy)-3,4-dihydroisoquinolin-1(2H)-one | ||
| Canonical SMILES | O=C1NCCC2=C(C=CC=C21)OCCCCN3CCCCC3 | ||
| Formula | C18H26N2O2 | M.Wt | 302.41 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.3068 mL | 16.5338 mL | 33.0677 mL |
| 5 mM | 661.4 μL | 3.3068 mL | 6.6135 mL |
| 10 mM | 330.7 μL | 1.6534 mL | 3.3068 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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.)
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 saline, 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.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 28 reference(s) in Google Scholar.)