product name Z-FA-FMK
Description: Z-FA-FMK, a control peptidic fluoromethylketone (boc-Thr-CH2F), is an irreversible cysteine protease inhibitor, and it also inhibits effector caspases. Z-FA-FMK can inhibit caspase activity in vitro and selectively inhibits recombinant effector caspases 2, -3, -6, and -7. In contrast, purified initiator caspases 8 and 10 are not affected, whereas the apoptosome-associated caspase 9 is only partially inhibited by Z-FA-FMK in vitro.
References: Anal Biochem. 1985 Sep;149(2):461-5; J Immunol. 2006 Sep 15;177(6):3827-36.
386.42
Formula
C21H23N2O4F
CAS No.
197855-65-5
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 77 mg/mL (199.3 mM)
Water: <1 mg/mL
Ethanol: 34 mg/mL (88.0 mM)
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19409762
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: 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. |
|---|---|
| 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. |
| Animal model | |
| Formulation & Dosage | |
| References | Anal Biochem. 1985 Sep;149(2):461-5; J Immunol. 2006 Sep 15;177(6):3827-36. |
