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In vitro: Apoptosis is a pathway of cell death orchestrated by a family of proteases called caspases. Boc-D-fmk inhibits TNFα-stimulated reactive oxygen species (ROS) generation. Boc-D-FMK inhibits apoptosis stimulated by TNF-α with an IC50 of 39 µM. BocD-fmk at 50 µM prevents genistein-induced apoptosis of p815 cells. Confocal microscopy shows that the release of mitochondrial apoptotic factors is inhibited by BocD-fmk. In vivo: Boc-D-FMK-fmk effectively attenuates the hepatocyte apoptosis in bile duct-ligated rats and may improve the survival rates after endotoxin challenge. A single injection of Boc-D-FMK results in longterm protection of MNs against root avulsion-induced death for more than 8 weeks and the Boc-D-FMK-treated MNs are able to regenerate their axons into an implanted PN graft and reinnervate the target muscle.
| Cell Experiment | |
|---|---|
| Cell lines | Neutrophils |
| Preparation method | Neutrophils (11.1 × 10^6 cells/mL) were cultured for 30 minutes in the presence or absence of 0.03-300 μM z-VAD-fmk or Boc-D-fmk before addition of TNFα (200 U/mL). Cells (100 μL) were added to a microtiter plate followed by an equal volume of lucigenin (0.25 mM for extracellular ROS release) or luminol (1 mM for intra- and extracellular ROS release). |
| Concentrations | 3-300 μM |
| Incubation time | 30 min |
| Animal Experiment | |
|---|---|
| Animal models | Male Sprague–Dawley rats |
| Formulation | DMSO |
| Dosages | 1.5 mg/kg |
| Administration | i.v. |
| Molecular Weight | 263.26 |
| Formula | C11H18FNO5 |
| CAS Number | 634911-80-1 |
| Solubility (25°C) | 125 mg/mL in DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Caspase Products |
|---|
| PAC-1
PAC-1 is a procaspase-activating compound; activates procaspase-3 to produce caspase-3 (EC50 = 0.22 μM). |
| MDK83190
MDK83190 (Apoptosis Activator 2) strongly induces caspase-3 activation, PARP cleavage, and DNA fragmentation which leads to the destruction of cells (Apaf-1 dependent) with IC50 of ~4 μM, inactive to HMEC, PREC, or MCF-10A cells. |
| LY573636 (Tasisulam)
LY573636 is a novel anticancer agent that induces apoptosis through the intrinsic pathway and has antiangiogenic activity in preclinical models. |
| Q-VD-OPh
Q-VD-OPh is a potent, irreversible pan-caspase inhibitor with IC50 ranging from 25 to 400 nM for caspases 1, 3, 8, and 9, showing inhibitory effects on terminal caspase activation, substrate cleavage, and DNA ladder formation associated with apoptosis. |
| Z-DEVD-FMK
Z-DEVD-FMK is a specific, irreversible Caspase-3 inhibitor with an IC50 of 18 μM, and also shows potent inhibition on caspase-6, caspase-7, caspase-8, and caspase-10. |
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