[Kamiya Biomedical] Biotin-FA-FMK (Cathepsin B Inhibitor)
Cat. No.: AD-012 (5 mg)
Chemical Name: Biotin-Phe-Ala-CH2F
Molecular Weight: 478
Description: Trifluoroacetic acid salt of the fluoromethyl ketone biotinylated peptide inhibitor of Cathepsin B (Caspase inhibitor negative control). The CH2F (fluoromethyl ketone) inhibitor has several advantages over other types of derivatives:
- Penetrates cell membranes
- Not toxic to cells
- Irreversible inhibition
Introduction: The ten known caspases are involved in the proteolytic cascade that results in apoptosis and in the maturation process of IL-1ß necessary for inflammation. The use of biotinylated FMK-type inhibitors for various caspases requires a biotinylated FMK-type inhibitor that does not affect caspases as a negative control. The Biotin-FA-FMK does not inhibit the activity of caspases in intact cells and does not block the induction of apoptosis as caspase inhibitors do. It can, therefore, be used as a negative control for the FMK moiety of the biotinylated caspase inhibitor, both in vivo and in vitro.
Specificity: Specifically binds to and inhibits Cathepsin B. Does not bind to or inhibit any of the caspases.
Form: Brown solid.
Applications: Irreversible binding to and inhibition of Cathepsin B. The second order rate constant (k2) of inactivation for human liver Cathepsin B is 1,220 M-1s -1, determined from the observed rate of inactivation (k) divided by the inhibitor concentration (I): k2 = k/I. Serves as a negative control in studies using the biotinylated FMK-containing caspase inhibitors.
