In vitro: Z-FA-FMK inhibits the degradation of fibrillar collagen by fibroblasts and osteoclasts. Z-FA-FMK inhibits LPS-induced cytokine production via inhibition of NF-kappaB-dependent gene expression in macrophages. Z-FA-FMK efficiently blocks T cell proliferation induced by mitogens and IL-2 in vitro.
In vivo: Z-FA-FMK significantly increases pneumococcal growth in both lungs and blood in a mouse model of intranasal pneumococcal infection. Z-FA-FMK blocks reovirus infection of Ras oncogenic tumours and host heart tissues in severe combined immunodeficiency mice.
| Cell Experiment | |
|---|---|
| Cell lines | PBMCs |
| Preparation method | T cell proliferation following mitogen stimulation is determined using [3H]thymidine incorporation. In brief, PBMCs or purified T cells are seeded in a 96-well plate and stimulated with either PHA (5 μg/ml), costimulated with anti-CD3 mAb (5 μg/ml) and anti-CD28 mAb (2.5 μg/ml) or PMA plus ionomycin in the presence or absence of z-FA-FMK. The cells are cultured for 72 h with the last 16 h pulsed with [methyl-3H]thymidine (0.037 MBq). The cells are harvested onto glass fiber filter mats using a Tomtec automated multiwell harvester. |
| Concentrations | ~100 μM |
| Incubation time | 72 h |
| Animal Experiment | |
|---|---|
| Animal models | SCID mice |
| Formulation | DMSO |
| Dosages | 0.02 mg/mouse |
| Administration | i.p. |
| Molecular Weight | 386.42 |
| Formula | C21H23FN2O4 |
| CAS Number | 197855-65-5 |
| Solubility (25°C) | 60 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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