Drug intelligence / Profile preview

Z-VDVAD-FMK

Development stage
Preclinical
Modality
Peptides, Small Molecules
Administration
Intravitreal, Intraperitoneal
01

Overview

Z-VDVAD-FMK is a cell-permeable, irreversible peptide inhibitor specifically designed to target **caspase-2**. It consists of the pentapeptide sequence Val-Asp-Val-Ala-Asp (VDVAD), which corresponds to the preferred cleavage site of caspase-2, conjugated to an N-terminal benzyloxycarbonyl (Z) protecting group and a C-terminal fluoromethylketone (FMK) reactive group. The FMK moiety acts as a Michael acceptor that forms a covalent bond with the active site cysteine residue of the protease, thereby permanently inactivating the enzyme. In biological research, Z-VDVAD-FMK is extensively utilized as a pharmacological tool to elucidate the role of caspase-2 in various apoptotic signaling pathways, including those induced by DNA damage, endoplasmic reticulum (ER) stress, and viral infections. Preclinical studies have explored its potential neuroprotective effects in models of stroke and retinal ganglion cell death, as well as its ability to modulate apoptosis in certain cancer cell lines and viral replication processes.

Other names
Caspase-2 Inhibitor IICaspase2 Inhibitor IICaspase 2 Inhibitor IIZ-Val-Asp-Val-Ala-Asp-FMKBenzyloxycarbonyl-Val-Asp-Val-Ala-Asp-fluoromethylketone
02

Targets

CASP2 (Caspase-2)

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