Name: Z-FA-FMK
Price: 450.00 USD

- Overview
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    Background
    
    Z-FA-FMK is a control peptidic fluoromethylketone (boc-Thr-CH2F), and inhibitor to calpain (Ac-Leu-Leu-norleucinal), cathepsin B (Z-Phe-Ala-CH2F), and CPP32-like proteases (Z-DEVD-CH2F) [1]. A peptidyl fluoromethyl ketone (cathepsin B) was found to be an effective compound in a time dependent inactivation of cathepsin B isozymes from a number of tissues including human tumors [2]. The inhibitor of cathepsins B and L Z-FA-fmk blocks the induction of DEVDase activity, DNA fragmentation, and externalization of phosphatidylserine by selective RRMs. 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. [3]
    It is an inhibitor of cysteine proteases, such as cathepsin B, which do not require a P1 Asp residue. It may be used as a negative control inhibitor for FMK P1 Asp caspase inhibitors.
    
    1. Inhibition of the interleukin-1 beta converting enzyme family rescues neurons from apoptotic death. Lynch, T., Vasilakos, J.P., Raser, K., Keane, K.M., Shivers, B.D. Mol. Psychiatry (1997)
    2. Visualization of time-dependent inactivation of human tumor cathepsin B isozymes by a peptidyl fluoromethyl ketone using a fluorescent print technique. Smith, R.E., Rasnick, D., Burdick, C.O., Cho, K.J., Rose, J.C., Vahratian, A. Anticancer Res. (1988)
    3. Lopez-Hernandez, F. J., Ortiz, M. A., Bayon, Y., & Piedrafita, F. J. (2003). Z-FA-fmk Inhibits Effector Caspases but not Initiator Caspases 8 and 10, and Demonstrates That Novel Anticancer Retinoid-related Molecules Induce Apoptosis via the Intrinsic Pathway1. Molecular cancer therapeutics, 2(3), 255-263.
- Properties
  - Alternative Name
    
    Z-FA-FMK, Z-Phe-Ala-fluoromethyl ketone, Z-Phe-Ala-FMK, Zfa-FMK, Z-Phe-Ala-CH2F, Cathepsin B, Caspase Inhibitor; benzyl N-[1-[(4-fluoro-3-oxobutan-2-yl)amino]-1-oxo-3-phenylpropan-2-yl]carbamate
    
    CAS Number
    
    105637-38-5;197855-65-5
    
    Molecular Formula
    
    C21H23N2O4F
    
    Molecular Weight
    
    386.42
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    insoluble in H2O; ≥13.45 mg/mL in DMSO; ≥3.57 mg/mL in EtOH with ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Mohammed Mohasin, Katharin Balbirnie-Cumming, et al. "Macrophages utilize mitochondrial fission to enhance mROS production during responses to Streptococcus pneumoniae." bioRxiv. 2019 August 02.
    2. Hodges AL, Kempen CG, et al. "TNF Family Cytokines Induce Distinct Cell Death Modalities in the A549 Human Lung Epithelial Cell Line when Administered in Combination with Ricin Toxin." Toxins (Basel). 2019 Aug 1;11(8). pii: E450. PMID:31374990

Z-FA-FMK

Z-FA-FMK

Background

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