MBD, a novel fluorescent probe (7-(p-Methoxybenzylamino)-4-nitrobenz-2,1,3-oxadiazole), is utilized to study the conformation of protein and nucleoprotein. Its application is extended to bacterial ribosomes, as well as bovine trypsinogen and trypsin. MBD exhibits significant fluorescence when it binds to the hydrophobic region of macromolecules [1][2].
MMP inhibitor I is a peptide inhibitor of matrix metalloproteinase-1 (MMP-1), MMP-2, and MMP-3 (IC50s = 1.3, 30, and 150 μM, respectively). It is selective for MMP-1, MMP-2, and MMP-3 over the proteases thermolysin, urease, trypsin, α-chymotrypsin, plasmin, and elastase at concentrations up to 4 mM.
CRA-2059 hydrochloride is a highly specific and selective tryptase inhibitor, with a Ki of 620 pM for recombinant human tryptase-β (rHTβ)[1][2]. Tryptase is a trypsin-like serine protease found as a major protein component in human mast cell secretory granules. CRA-2059 hydrochloride has the potential for inflammatory bowel disease research[1]. [1]. Tremaine WJ, et al. Treatment of mildly to moderately active ulcerative colitis with a tryptase inhibitor (APC 2059): an open-label pilot study. Aliment Pharmacol Ther. 2002;16(3):407-413.[2]. Selwood T, et al. Potent bivalent inhibition of human tryptase-beta by a synthetic inhibitor. Biol Chem. 2003;384(12):1605-1611.
CRA-2059 is a highly specific and selective tryptase inhibitor, with a Ki of 620 pM for recombinant human tryptase-β (rHTβ)[1][2]. Tryptase is a trypsin-like serine protease found as a major protein component in human mast cell secretory granules. CRA-2059 has the potential for inflammatory bowel disease research[1]. [1]. Tremaine WJ, et al. Treatment of mildly to moderately active ulcerative colitis with a tryptase inhibitor (APC 2059): an open-label pilot study. Aliment Pharmacol Ther. 2002;16(3):407-413.[2]. Selwood T, et al. Potent bivalent inhibition of human tryptase-beta by a synthetic inhibitor. Biol Chem. 2003;384(12):1605-1611.
Suomilide effectively inhibits human trypsin-2 and trypsin-3, displaying IC50 values of 4.7 nM and 11.5 nM, respectively. Additionally, it exhibits inhibition of trypsin-1 with an IC50 value of 104 nM.
Calmodulin antagonist-1 (W-7) is a calmodulin (CaM) antagonist that effectively inhibits calmodulin-activated Ca 2+ -phosphodiesterase (PDE) with an IC 50 of 28 μM. This compound also competitively inhibits trypsin-treated Ca 2+ -PDE with respect to cyclic GMP, exhibiting an IC 50 of 375 μM and a K i value of 300 μM.