Boc-LRR-AMC is a fluorogenic substrate for the trypsin-like activity of the 26S proteasome or 20S proteolytic core. Upon enzymatic cleavage by the 26S proteasome or 20S proteolytic core, amino-4-methylcoumarin (AMC) is released and its fluorescence can be used to quantify 26S proteasome or 20S proteolytic core trypsin-like activity. AMC displays excitation emission maxima of 340-360 440-460 nm, respectively.
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.
APC-6860 is a trypsin-like serine proteases inhibitor with k i values of 0.21, 0.44, 1.5, 16.8, 20, 30 μM for uPA, trypsin, tryptase, tPA, thrombin and factor Xa, respectively. APC-6860 has a selectivity ratio for tPA versus uPA of 80. APC-6860 has k i values of 0.1, 0.082 μM for human and murine urokinases, respectively. APC-6860 can be used for the research of cancer.