Q-VD(OMe)-OPh
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. 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
- 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
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Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 527 |
Formula | C26H25F2N3O6 |
Synonyms | Q-VD(OMe)-OPh |
Solubility | ≥26.35 mg/mL in DMSO; insoluble in H2O; ≥97.4 mg/mL in EtOH |
Chemical Name | (S)-methyl 5-(2,6-difluorophenoxy)-3-((S)-3-methyl-2-(quinoline-2-carboxamido)butanamido)-4-oxopentanoate |
SDF | Download SDF |
Canonical SMILES | O=C(N[C@@H](C(C)C)C(N[C@@H](CC(OC)=O)C(COC1=C(F)C=CC=C1F)=O)=O)C2=NC3=CC=CC=C3C=C2 |
Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
General tips | We do not recommend long-term storage for the solution, please use it up soon. |
Cell experiment:[1] | |
Cell lines |
Acute myeloid leukemia (AML) blasts |
Reaction Conditions |
5 μM Q-VD-OPh for 7 d incubation |
Applications |
Caspase inhibitor Q-VD-OPh induced cell differentiation, and further enhanced differentiation of AML blasts when combined with vitamin D derivatives. Q-VD-OPh alone was also able to increase the expression of differentiation markers in these AML blasts. |
Animal experiment:[2] | |
Animal models |
A murine model of stroke induced by middle cerebral artery occlusion (MCAO) |
Dosage form |
500 μg Administered intraperitoneally |
Applications |
Q-VD-OPh reduced ischemic brain damage and stroke-induced programmed cell death in thymus and spleen, decreased susceptibility to post-stroke bacteremia, and improved survival. |
Note |
The technical data provided above is for reference only. |
References: 1. Chen-Deutsch X, Kutner A, Harrison JS, et al. The pan-caspase inhibitor Q-VD-OPh has anti-leukemia effects and can interact with vitamin D analogs to increase HPK1 signaling in AML cells. Leukemia Research, 2012, 36(7): 884-888. 2. Braun JS, Prass K, Dirnagl U, et al. Protection from brain damage and bacterial infection in murine stroke by the novel caspase-inhibitor Q-VD-OPH. Experimental Neurology, 2007, 206(2): 183-191. |
Quality Control & MSDS
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