Home>>Signaling Pathways>> Proteases>> Caspase>>Q-VD-OPh hydrate

Q-VD-OPh hydrate (Synonyms: Quinoline-Val-Asp-Difluorophenoxymethyl Ketone)

Catalog No.GC16316

A caspase inhibitor with low cytotoxicity

Products are for research use only. Not for human use. We do not sell to patients.

Q-VD-OPh hydrate Chemical Structure

Cas No.: 1135695-98-5

Size Price Stock Qty
10mM (in 1mL DMSO)
$175.00
In stock
1mg
$65.00
In stock
5mg
$160.00
In stock
10mg
$291.00
In stock
25mg
$582.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

View current batch:

Protocol

Cell experiment[1]:

Cell lines

JURL-MK1 and HL60 cell

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reaction Conditions

No specific suggestion

Applications

Q-VD-OPh largely inhibited caspase-3 and 7 activity at 0.05 mM. Caspase-8 was also inhibited by Q-VD-OPh at very low concentration. Q-VD-OPh prevented the cleavage of PARP-1 at 10 mM . Q-VD-OPh inhibited DNA fragmentation and disruption of the cell membrane functionality at 2 mM, and the drug-induced loss of cellular adhesivity to fibronectin need 10 mM Q-VD-OPh.

Animal experiment [2]:

Animal models

TgCRND8 mice in 3 months-old

Dosage form

Intraperitoneally Injected with 10 mg/kg QVD-OPh at 3 times a week for 3 months

Applications

Q-VD-OPh inhibited caspase-7 activation and limited the pathological changes of tau and caspase cleavage in chronic treatment of Alzheimer disease.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

1. Kuželová K1, Grebeňová D, Brodská B.Dose-dependent effects of the caspase inhibitor Q-VD-OPh on different apoptosis-related processes. J Cell Biochem. 2011 Nov;112(11):3334-42.

2. Rohn TT, Kokoulina P, Eaton CR et al. Caspase activation in transgenic mice with Alzheimer-like pathology: results from a pilot study utilizing the caspase inhibitor, Q-VD-OPh.  Int J Clin Exp Med. 2009 Nov 5;2(4):300-8.

Background

The broad spectrum caspase inhibitor, QVD-OPh, provides a cost effective, non toxic, and highly specific means of apoptotic inhibition and provides new insight into the design of new inhibitors1.

Actinomycin D rapidly induced apoptosis and this was dramatically inhibited by the caspase inhibitor, Q-VD-OPh (quinolyl-valyl-O-methylaspartyl-[-2, 6-difluorophenoxy]-methyl ketone). Q-VD-OPh was significantly more effective in preventing apoptosis than the widely used inhibitors, ZVAD-fmk and Boc-D-fmk. Q-VD-OPh was also equally effective in preventing apoptosis mediated by the three major apoptotic pathways, caspase 9/3, caspase 8/10, and caspase 12. In addition to the increased effectiveness, Q-VD-OPh was not toxic to cells, even at high concentrations.

Q-VD-OPh was equally effective at inhibiting the three major apoptotic pathways, was functional in different cell types and species (human, mouse, and rat) and prevented terminal caspase activation, substrate cleavage, and DNA ladder formation associated with apoptosis. Q-VD-OPh can inhibit recombinant caspases 1, 3, 8, and 9 with IC50 values ranging from 25 to 400 nM2. The effectiveness of Q-VD-OPh as an apoptotic inhibitor is evidenced by the complete suppression of an apoptotic inducer capable of inducing substantial cell death in less than 4 hours.

Q-VD-OPh protected against the substantial apoptosis induced by actinomycin D. In addition, Q-VD-OPh alone exhibited little or no toxicity, even at extremely high concentrations.

The effective concentration of Q-VD-OPh may provide a unique reagent when trying to revive hard to propagate cell lines from liquid nitrogen. The addition of this inhibitor to thawed cells would give the cells adequate time to recover, even in the presence of standard DMSO concentrations (10%), from the stress of thawing and begin to proliferate in the absence of toxicity. Q-VD-OPh is stable in solution for several months and is effective in culture for at least 2.5 days. This would provide an ideal time frame for cell recovery; whereas, the subsequent decrease in effectiveness over time would be fortuitous in that the cells would return to standard culture conditions with minimal manipulation1.

References:
1. T. M. Caserta, A. N. Smith, A. D. Gultice, M. A. Reedy and T. L. Brown, Q-VD-OPh, a broad spectrum caspase inhibitor with potent antiapoptotic properties, Apoptosis 2003; 8: 345–352
2. Yin XM. Signal transduction mediated by Bid, a pro-death Bcl-2 family proteins, connects the death receptor and mitochondria apoptosis pathways. Cell Res 2000; 10: 161–167

Chemical Properties

Cas No. 1135695-98-5 SDF
Synonyms Quinoline-Val-Asp-Difluorophenoxymethyl Ketone
Chemical Name (3S)-5-(2,6-difluorophenoxy)-3-[[(2S)-3-methyl-2-(quinoline-2-carbonylamino)butanoyl]amino]-4-oxopentanoic acid
Canonical SMILES CC(C)C(C(=O)NC(CC(=O)O)C(=O)COC1=C(C=CC=C1F)F)NC(=O)C2=NC3=CC=CC=C3C=C2
Formula C26H25F2N3O6.xH2O M.Wt 513.49
Solubility ≥ 25.6745mg/mL 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.

Complete Stock Solution Preparation Table

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 1.9475 mL 9.7373 mL 19.4746 mL
5 mM 0.3895 mL 1.9475 mL 3.8949 mL
10 mM 0.1947 mL 0.9737 mL 1.9475 mL
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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.
3. All of the above co-solvents are available for purchase on the GlpBio website.

Reviews

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Average Rating: 5 ★★★★★ (Based on Reviews and 30 reference(s) in Google Scholar.)

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