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Z-FA-FMK Cysteine proteases inhibitor

Catalog No.A8170
Size Price Stock Qty
10mM (in 1mL DMSO)
$250.00
In stock
Evaluation Sample
$28.00
In stock
1mg
$60.00
In stock
5mg
$200.00
In stock
10mg
$360.00
In stock
25mg
$400.00
In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

Z-FA-FMK

Biological Activity

Description Z-FA-FMK is an irreversible inhibitor of cysteine protease
Targets cysteine protease          
IC50            

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Chemical Properties

Cas No. 105637-38-5 SDF Download SDF
Synonyms Z-FA-FMK, Z-Phe-Ala-fluoromethyl ketone, Z-Phe-Ala-FMK, Zfa-FMK, Z-Phe-Ala-CH2F, Cathepsin B, Caspase Inhibitor
Chemical Name benzyl N-[1-[(4-fluoro-3-oxobutan-2-yl)amino]-1-oxo-3-phenylpropan-2-yl]carbamate
Canonical SMILES CC(C(=O)CF)NC(=O)C(CC1=CC=CC=C1)NC(=O)OCC2=CC=CC=C2
Formula C21H23N2O4F M.Wt 386.42
Solubility >13.45mg/mL in DMSO Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

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.

References:
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.