Substrates and Inhibitors

A fluorogenic substrate for caspase 3. The 7-amido-4-trifluoromethylcoumarin derivatives have better membrane permeability than the 7-amido-4-methylcoumarin derivatives.

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

Cleavage of R110 peptides by caspases generates strongly fluorescent R110 that can be monitored fluorimetrically at 510-530 nm with excitation of 488 nm.This R110 substrate is specific for caspases 3 and 7.

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...

PI/PS (4:1, w/w) unilamellar vesicle, prepared with L-alpha-phosphatidylinositol (Liver, Bovine) (sodium salt) and L-alpha-phosphatidylserine (Brain, Porcine) (sodium salt). Lipid monolayer was formed by sonication. Application: Useful as a substrate for PI-3 kinase activity assays and other lipid kinases....

(BOC-VPR)2R110 is a sentive fluorogenic substrate for alpha-thrombin. The non-fluorescent substrate generates a bright green fluorescent R110 product that has Ex/Em = 495/520 nm, and can be easily detected with the FITC filter set. This substrate has also been used for the rapid detection of MRSA...

Proteinase 3 (PR3, myeloblastin) is a polymorphonuclear leukocyte serine proteinase that degrades matrix proteins including fibronectin, laminin, vitronectin, and collagen type IV to generate antimicrobial peptides. Neutrophil elastase is a serine proteinase that is secreted by neutrophils during inflammation to...

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...

Bortezomib is a dipeptide boronic acid derivative that reversibly inhibits the 20S proteasome (Ki = 0.6 nM). It binds the beta5-subunit of the 20S proteasome and selectively inhibits chymotryptic activity. In part by blocking the degradation of tumor-suppressing and proapoptotic proteins, bortezomib drives cell...

An inhibitor of acid proteases isolated from streptomyces. It has been shown to induce contractile effects on rat aorta rings.

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...