Substrates and Inhibitors

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...

Furin is a proprotein convertase, converting precursor proteins to functional proteins within the Golgi/trans-Golgi secretory pathway. Furin inhibitor I is a selective, irreversible, and cell-permeable competitive inhibitor of proprotein convertases, including furin/SPC1 (Ki = ~1 nM), SPC2/PC2 (Ki = 0.36 nM),...

MCL-1 Peptide Ligand is useful as a substrate for screening services and optimized for use with the following TR-FRET assay kits: * MCL-1 TR-FRET Assay kit (BPS-79506) * MCL-1 TR-FRET Assay kit (Mouse) (BPS-79928)

A reversible inhibitor of IL-1 converting enzyme (ICE), inhibits poly(ADP-ribose) polymerase cleavage by apopain (caspase 3).

Z-VDVAD-FMK is a peptide caspase-2 inhibitor. Intravitreal injection of Z-VDVAD-FMK (4,000 ng/ml) reduces optic nerve crushing-induced retinal ganglion cell apoptosis in rats. It also prevents endothelial cell apoptosis in a dog model of subarachnoid hemorrhage-induced chronic cerebral vasospasm. InChI:...

Z-VEID-FMK is a peptide inhibitor of caspase-3 and -6 (apparent IC50s = 45. and 128. nM, respectively). It decreases lamin cleavage induced by caspase-6 in a cell-free assay (IC50 = 45 µM). Z-VEID-FMK (160 µM) decreases apoptosis in primary human erythroblasts cultured in erythropoietin-deficient media. It increases...

A colorimetric substrate for caspase 3, a protease that is rapidly activated when cells are exposed to apoptotic conditions and that cleaves poly(ADP-ribose) polymerase.

Purity: >98% (HPLC). Rev. inhibitor of aspartic proteinases, e.g. cathepsin D, renin, pepsin, bacterial aspartic proteinases and HIV protease. Soluble in MeOH or EtOH at 1 mg/ml, stable for 1 week at 4 °C. Eff. conc.: 1-5 µM.

Pepstatin A is a bacteria-derived pentapeptide inhibitor of aspartic proteases. It inhibits pepsin, cathepsin D, and HIV protease (IC50s = 50s = 0.32 and 15 µM for the porcine and human enzymes, respectively). It inhibits HIV replication in infected H9 cells when used at a concentration of 100 µM and inhibits...

The non-fluorescent R110 substrates generate the bright green fluorescent rhodamine 110 product that has Ex/Em = 494/521 nm, and can be easily detected with a FITC filter set. In general, R110 substrates are much more sensitive than the AMC-, AFC- or 4-nitroaniline-based substrates. This R110 substrate is used for...

Ac-LEVD-AFC is a fluorogenic substrate for caspase-4. Upon enzymatic cleavage by caspase-4, 7-amino-4-trifluoromethylcoumarin (AFC) is released and its fluorescence can be used to quantify caspase-4 activity. AFC displays excitation/emission maxima of 400/505 nm, respectively.Formal Name:...

D-Val-Leu-Lys-p-nitroanilide is a selective colorimetric substrate for plasmin used to determine the formation of plasmin from plasminogen in amidolytic activity assays and plasminogen activating assays. Plasmin is a plasma serine protease whose main role is to dissolve fibrin blood clots. After cleavage by plasmin...