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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related Caspase Products |
|---|
| TC11
TC11 is a phenylphthalimide derivative and an activator of caspase-9 and CDK1, as well as a degrader of MCL1.TC11 is structurally related to immunomodulatory active molecules. During prolonged mitotic blockade, TC11 induces MCL1 degradation and leads to apoptotic death. |
| Ac-Ile-Glu-Thr-Asp-pNA
Ac-Ile-Glu-Thr-Asp-pNA is a substrate for caspase-8. |
| Z-DEVD-AFC
Z-DEVD-AFC is a cell-permeant substrate for caspase-3, which causes a shift in fluorescence uponcleavage of the AFC fluorophore. |
| Ac-IETD-AFC
Ac-IETD-AFC is a fluorogenic substrate of caspase-8, caspase-3, caspase-10, and granzyme B. |
| Z-VDVAD-FMK
Z-VDVAD-FMK is a special inhibitor of caspase-2. |
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