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Q-VD(OMe)-OPh Pan-caspase inhibitor

Catalog No.A8165
Size Price Stock Qty
10mM (in 1mL DMSO)
$570.00
In stock
Evaluation Sample
$28.00
In stock
1mg
$110.00
In stock
5mg
$300.00
In stock
10mg
$500.00
In stock
25mg
$800.00
In stock

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Email: [email protected]

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Sample solution is provided at 25 µL, 10mM.

Product Citations

1. Burman JL, Pickles S, et al. "Mitochondrial fission facilitates the selective mitophagy of protein aggregates." J Cell Biol. 2017 Oct 2;216(10):3231-3247. PMID:28893839
2. Gong YN, Guy C, et al. "ESCRT-III Acts Downstream of MLKL to Regulate Necroptotic Cell Death and Its Consequences." Cell. 2017 Apr 6;169(2):286-300.e16. PMID:28388412
3. Wang L, Mehta S, et al. "Inhibition of Murine Pulmonary Microvascular Endothelial Cell Apoptosis Promotes Recovery of Barrier Function under Septic Conditions." Mediators Inflamm. 2017;2017:3415380. PMID:28250575
4. Rodriguez, D. A, et al. "Characterization of RIPK3-mediated phosphorylation of the activation loop of MLKL during necroptosis." Cell Death & Differentiation (2015). PMID:26024392
5. Milasta S, Dillon CP, et al. "Apoptosis-Inducing-Factor-Dependent Mitochondrial Function Is Required for T Cell but Not B Cell Function." Immunity. 2016 Jan 19;44(1):88-102. PMID:26795252

Quality Control

Chemical structure

Q-VD(OMe)-OPh

Related Biological Data

Q-VD(OMe)-OPh

Related Biological Data

Q-VD(OMe)-OPh

Related Biological Data

Q-VD(OMe)-OPh

Related Biological Data

Q-VD(OMe)-OPh

Related Biological Data

Q-VD(OMe)-OPh

Related Biological Data

Q-VD(OMe)-OPh

Related Biological Data

Q-VD(OMe)-OPh

Biological Activity

Description Q-VD(OMe)-Oph is an inhibitor of caspase.
Targets Caspase          
IC50            

Protocol

Cell experiment [1]:

Cell lines

The mouse immature B cell WEHI 231 immature cell lines

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

4 h; 50 μg/mL

Applications

To analyze the effects of broad spectrum caspase inhibitors on actinomycin D-induced apoptosis in WEHI 231 cells, DNA fragmentation was analyzed after 4 h, when substantial apoptosis, in the absence of caspase inhibitors, had occurred. Incubation with decreasing doses of or Q-VD-OPh in the presence of 1µg/ml actinomycin D indicated that the compound exhibited a dose dependent inhibition of apoptosis.

Animal experiment [2]:

Animal models

P7 rats

Dosage form

1 mg/kg; intraperitoneal injection.

Applications

Q-VD-OPh attenuates brain injury after neonatal stroke. P7 rats underwent electrocoagulation of the left middle cerebral artery and transient homolateral common carotid artery occlusion for 50 min followed by 48 h of recovery. A single injection of Q-VD-OPh significantly reduced by 48% the infarct volume as compared with control ischaemic animals (12.6 ± 2.8, n=16, p=0.006) and no rat died. Q-VD-OPh also induced a clear decrease in the number of TUNEL-positive cells versus vehicle-treated animals.

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] Caserta T M, Smith A N, Gultice A D, et al. Q-VD-OPh, a broad spectrum caspase inhibitor with potent antiapoptotic properties[J]. Apoptosis, 2003, 8(4): 345-352.

[2] Renolleau S, Fau S, Goyenvalle C, et al. Specific caspase inhibitor Q‐VD‐OPh prevents neonatal stroke in P7 rat: a role for gender[J]. Journal of neurochemistry, 2007, 100(4): 1062-1071.

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Chemical Properties

Cas No. SDF Download SDF
Synonyms Q-VD(OMe)-OPh
Chemical Name (S)-methyl 5-(2,6-difluorophenoxy)-3-((S)-3-methyl-2-(quinoline-2-carboxamido)butanamido)-4-oxopentanoate
Canonical SMILES O=C(N[[email protected]@H](C(C)C)C(N[[email protected]@H](CC(OC)=O)C(COC1=C(F)C=CC=C1F)=O)=O)C2=NC3=CC=CC=C3C=C2
Formula C26H25F2N3O6 M.Wt 527
Solubility >26.4mg/mL in DMSO Storage Store at -20°C
Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Background

Q-VD-OPh (quinolyl-valyl-O-methylaspartyl-[-2,6-difluorophenoxy]-methyl ketone) is a broad spectrum caspase inhibitor,  provides a cost effective, non toxic, and highly specific means of apoptotic inhibition and provides new insight into the design of new inhibitors. [1] It is significantly more effective in preventing apoptosis than the widely used inhibitors, ZVAD-fmk and Boc-D-fmk. Q-VD-OPh is 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 is equally effective at inhibiting the three major apoptotic pathways, it 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. [2] 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.

Ref:

  1. 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