Substrate und Inhibitoren

Z-AEVD-FMK is an irreversible inhibitor of caspase-10 and related caspases. At 10 µM, it can prevent the initiation of Fas signaling by caspase-10 in Jurkat T lymphoma cells, preventing Bid cleavage into its active form, caspase cascade activation, and apoptosis.

Ac-LETD-AFC is a fluorogenic substrate that can be cleaved specifically by caspase-8. Caspase activity can be quantified by fluorescent detection of free AFC (also known as 7-amino-4-trifluoromethylcoumarin), which is excited at 400 nm and emits at 505 nm.

Histone H3 (23-34) is a peptide fragment of histone H3 that corresponds to amino acid residues 24-35 of the human histone H3.1 and H3.2 sequences. It contains lysine residues at positions 23 and 27 that are subject to methylation and acetylation and have a role in the regulation of gene expression and a serine...

Histone H3 (69-89) amide is a peptide fragment of histone H3 that corresponds to amino acid residues 70-90 of the human histone H3.1 and H3.2 sequences. Histone H3 (69-89) amide contains a lysine residue at position 79 that is subject to methylation and acetylation and has a role in regulation of gene expression.

Bz-IEGR-pNA is a colorimetric substrate for Factor Xa. Factor Xa preferentially binds to and cleaves the Ile-Glu-Gly-Arg (IEGR) peptide sequence to release p-nitroanilide (pNA), which can be quantified by colorimetric detection at 405 nm as a measure of Factor Xa activity.

alpha-Bungarotoxin is a snake venom-derived toxin that irreversibly binds nicotinic acetylcholine receptors (Ki = ~2.5 µM in rat) present in skeletal muscle, blocking action of acetylcholine at the postsynaptic membrane and leading to paralysis. It has been widely used to characterize activity at the neuromuscular...

Abz-Ala-Pro-Glu-Glu-Ile-Met-Arg-Arg-Gln-EDDnp is a fluorescence-quenched peptide substrate for human neutrophil elastase (kcat/Km = 531 mM-1s-1). Enzymatic peptide hydrolysis disrupts the Abz:EDDnp donor-acceptor pair allowing fluorescence measurement of Abz (ex = 320 nm, em = 420 nm).

Abz-Val-Ala-Asp-Nva-Arg-Asp-Arg-Gln-EDDnp is a fluorescence-quenched peptide substrate for human proteinase 3 (kcat/Km = 1,570 mM-1s-1). Enzymatic peptide hydrolysis disrupts the Abz:EDDnp donor-acceptor pair allowing fluorescence measurement of Abz (ex = 320 nm, em = 420 nm).

Aeruginosins are tetrapeptides isolated from cyanobacteria such as Microcystis aeruginosa. Like other cyanotoxins, aeruginosins inhibit serine/threonine protein phosphatases (PPs). In endothelial cells, aeruginosins decrease levels of IL-8 and ICAM-1 and inhibit NF-kappaB activity. Aeruginosins may also bind...

Aeruginosamides are linear ribosomal peptides isolated from cyanobacteria such as Microcystis aeruginosa. Like other cyanotoxins, aeruginosamides may inhibit serine/threonine protein phosphatases (PPs) or exhibit antithrombotic activity.

Aeruginosamides are linear ribosomal peptides isolated from cyanobacteria such as Microcystis aeruginosa. Like other cyanotoxins, aeruginosamides may inhibit serine/threonine protein phosphatases (PPs) or exhibit antithrombotic activity.

Aeruginosamides are linear ribosomal peptides isolated from cyanobacteria such as Microcystis aeruginosa. Like other cyanotoxins, aeruginosamides may inhibit serine/threonine protein phosphatases (PPs) or exhibit antithrombotic activity.