Caspase-6抑制剂
When compared to other caspase inhibitors, Z-DRHD-FMK inhibited caspase 6 activity more effectively than the general caspase inhibitor Z-Val-Ala-Asp (OMe)-fluoromethy ketone (Z-VAD-FMK) or the caspase 6 inhibitor Z-Val-Glu(Ome)-Ile-Asp(OMe)-fluoromethyl ketone (Z-VEID-FMK). However, it was less effective in inhibiting TNFα-induced apoptosis than Z-VAD-FMK or Z-VEID-FMK, presumably because caspase 6 is only one of at least three effector caspases, the others being caspase 3 and 7, that are active during caspase dependent apoptosis. Loss of DNA-binding activity and TNFα-induced apoptosis can be prevented by caspase-6-preferred inhibitor (Z-VEID-FMK)1.
The caspase-6-specific inhibitor Z-VEID- FMK and general caspase inhibitors significantly prevent apoptosis of caspase-6-microinjected neurons2.
Z-VEID-FMK, which inhibits caspase-6, was also able to abolish the cleavage of procaspase-8, although caspase-6 is activated downstream of caspase-8 in Fas-mediated apoptosis3.
参考文献:
1. Nyormoi?et al?(2003) Sequence-based discovery of a synthetic peptide inhibitor of caspase 6. Apoptosis?8?371.
2. Y. Zhang C. Goodyer, Selective and Protracted Apoptosis in Human Primary Neurons Microinjected with Active Caspase-3, -6, -7, and -8. The Journal of Neuroscience, 2000, 20(22):8384–8389
3. Microinjected with Active Caspase-3, -6, -7, and -8 Taimen and Kallajoki?(2003) NuMA and nuclear lamins behave differently in Fas-mediated apoptosis. J.Cell Sci.116?571.
| Cell experiment [1]: | |
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Cell lines |
Luteal cells |
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Preparation method |
Soluble in DMSO. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reaction Conditions |
50 μM; 6 h |
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Applications |
Incubation of luteal cells in the presence of inhibitors of caspase-3 (Z-DEVD-FMK), caspase-6 (Z-VEID-FMK), caspase-8 (Z-IETD-FMK) and a general caspase inhibitor (Boc-DFMK) resulted in a reduction in the level of TNFα-induced DNA fragmentation. |
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参考文献: [1]. Abdo M1, Hisheh S, Dharmarajan A. Role of tumor necrosis factor-alpha and the modulating effect of the caspases in rat corpus luteum apoptosis. Biol Reprod. 2003 Apr;68(4):1241-8. | |
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