proteinase k

Proteinase K (Protease K) 是一种非特异性丝氨酸蛋白酶，可以耐受 SDS、尿素、pH 值 (4-12)、盐浓度和温度变化。Proteinase K 可水解多种肽键，用于蛋白消化。

Recombinant Proteinase K为一种serine protease，专门裂解脂肪族及芳香族氨基酸的羧基端肽键，适用于蛋白质消化与清除核酸制剂中的污染。

MeOSuc-AAPF-CMK (MeOSuc-Ala-Ala-Pro-Phe-CH2Cl) 是蛋白酶 K 抑制剂，具有较高效能。

PAR2 (1-6) amide is a synthetic peptide agonist of proteinase-activated receptor 2 (PAR2) that corresponds to residues 1-6 of the amino terminal tethered ligand sequence of human PAR2 and residues 37-42 of the full-length sequence.1It binds to NCTC 2544 cells expressing human PAR2 (Ki= 9.64 μM in a radioligand binding assay) and induces calcium mobilization in the same cells (EC50= 0.075 μM).2PAR2 (1-6) amide (100 μM) reduces colony formation of A549 lung cancer cells.1It induces superoxide production and degranulation in isolated human eosinophils when used at a concentration of 500 μM.3PAR2 (1-6) amide (5 μmol/kg) induces tear secretion in rats when used in combination with amastatin .4 1.Bohm, S.K., Kong, W., Bromme, D., et al.Molecular cloning, expression and potential functions of the human proteinase-activated receptor-2Biochem. J.314(Pt 3)1009-1016(1996) 2.Kanke, T., Ishiwata, H., Kabeya, M., et al.Binding of a highly potent protease-activated receptor-2 (PAR2) activating peptide, [3H]2-furoyl-LIGRL-NH2, to human PAR2Br. J. Pharmacol.145(2)255-263(2005) 3.Miike, S., McWilliam, A.S., and Kita, H.Trypsin induces activation and inflammatory mediator release from human eosinophils through protease-activated receptor-2J. Immunol.167(11)6615-6622(2001) 4.Nishikawa, H., Kawai, K., Tanaka, M., et al.Protease-activated receptor-2 (PAR-2)-related peptides induce tear secretion in rats: Involvement of PAR-2 and non-PAR-2 mechanismsJ. Pharmacol. Exp. Ther.312(2)324-331(2005)

Poly-D-lysine hydrobromide (MW 30000-70000)(Poly-D-lysine HBr) 是一种可口服的肽类 CaSR 激动剂，可从朊病毒感染的 SN56 神经母细胞瘤细胞中去除蛋白酶 K 抗性的 PrP。

Rivulariapeptolides 1155 是一种有效的丝氨酸蛋白酶 (serine protease) 抑制剂，对糜蛋白酶、弹性蛋白酶、蛋白蛋白酶 K 的 IC50分别为 41.84、4.94、56.54 nM。

NK314 is a novel synthetic benzo[c]phenanthridine alkaloid that shows strong antitumor activity. It inhibited topoisomerase II activity and stabilized topoisomerase II-DNA cleavable complexes. The DNA breaks occurred within 1h after treatment with NK314 even without digestion of topoisomerase II by proteinase K, whereas etoposide required digestion of the enzyme protein in cleavable complex to detect DNA breaks. Pretreatment with topoisomerase II catalytic inhibitors, ICRF-193 and suramin, reduced both cleavable complex-mediated DNA breaks and proteinase K-independent DNA breaks, but protease inhibitors and nuclease inhibitors only decreased the latter.

K-14585 is a proteinase-activated receptor 2 antagonist. K-14585 inhibited PAR(2)-mediated p65 NFkappaB phosphorylation and NFkappaB-DNA binding. K-14585 inhibited SLIGKV-stimulated IL-8 production, but given alone increased IL-8.

Digalacturonic acid，果胶或果胶酸的代谢产物，可用于蛋白酶 K 等酶的共结晶。

Rivulariapeptolides 988作为一种高效选择性丝氨酸蛋白酶抑制剂，对胰凝蛋白酶、弹性蛋白酶和蛋白酶K的IC50分别为95.46 nM、15.29 nM和85.50 nM。

Abz-Val-Ala-Asp-Nva-Arg-Asp-Arg-Gln-EDDnp 用作检测人类蛋白酶 3 (PR3) 活性的荧光猝灭肽底物，其比活性常数 (kcat Km) 为 1,570 mM-1s-1。

Rivulariapeptolides 1185 是一种高效的选择性丝氨酸蛋白酶抑制剂，其对胰凝蛋白酶、弹性蛋白酶和蛋白酶 K 的 IC50分别为 13.17 nM、23.59 nM 和 55.26 nM。

Rivulariapeptolides 1121，作为一种高效的选择性丝氨酸蛋白酶抑制剂，对胰凝蛋白酶、弹性蛋白酶和蛋白酶K展示出了显著的抑制活性，其IC50值分别为35.52 nM、13.24 nM和48.05 nM。

Molassamide B，丝氨酸蛋白酶抑制剂，对胰凝乳蛋白酶、弹性蛋白酶及蛋白酶 K 具有显著抑制活性，其IC50值分别为24.65、11.69和5.42 nM。