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Comment
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The novel Q-VD-OPH (Quinoline-Val-Asp-CH2-OPh) compound is an irreversible caspase inhibitor specifically designed for animal in vivo research. The Q-VD-OPH irreversibly binds to activated caspases to block apoptosis. Q-VD-OPH penetrates the bloodbrain barrier. The “OPH” trap with its superior potency, proven cell permeability and minimal toxicity provides an exceptional alternative to the fluoromethyl ketone family of inhibitors. The improvements derive from significant changes in structural design and replacement of the putatively toxic fluoromethyl ketone (FMK) with the non-toxic 2,6-difluorophenoxy (OPH) group. The mechanism of action involves the formation of an irreversible thioether bond between the aspartic acid derivative in the inhibitor and the active site cysteine of the caspase with the displacement of the 2,6-difluorophenoxy leaving group.
The “OPH” trap features:
- Non-toxic: A preliminary study showed no evidence of toxicity in mice injected with >1,000 mg/kg
- Potency: IC50 values against purified caspases are in the nanomolar range, over 90% inhibition of apoptosis when used in an in vitro cell-based assay
Prepare desired concentrated stocks solutions as follows: For each mg of Q-VD-OPH
20 mM - add 97 μL DMSO.
10 mM - add 194 μL DMSO.
5 mM - add 388 μL DMSO.
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