Pan-caspase inhibitor
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:
| Cell experiment [1]: | |
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Cell lines |
The mouse immature B cell WEHI 231 immature cell lines |
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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. |
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Reaction Conditions |
4 h; 50 μg/mL |
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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]: | |
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Animal models |
P7 rats |
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Dosage form |
1 mg/kg; intraperitoneal injection. |
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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. |
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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. |
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参考文献: [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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