trypsin-1

Diminazene aceturate 是血管紧张素转化酶 2 的激活剂，具有强效抗炎特性。它还是一种抗锥虫药物，适用于牲畜。它主要生化机理是通过与富含腺嘌呤-胸腺嘧啶碱基对的位点发生特异性相互作用，以非插入方式与锥虫动子体 DNA 结合。

4-Aminobenzamidine dihydrochloride (p-Aminobenzamidine dihydrochloride) 是一种强胰蛋白酶 (trypsin)抑制剂，也是一种相对较弱的尿激酶型纤溶酶原激活剂 (uPA) 抑制剂 (Ki=82 μM)。4-Aminobenzamidine 可抑制 SCID 小鼠体内前列腺肿瘤的生长。

Patamostat (E-3123)是一种有效的蛋白酶抑制剂，对胰蛋白酶、纤溶酶和凝血酶具有显著抑制效果，其IC50值分别为39 nM、950 nM和1.9 μM。Patamostat可能在急性胰腺炎的发病机制和发展中发挥抑制作用。

VR23 是一种蛋白酶体抑制剂，对胰蛋白酶样蛋白酶体、糜蛋白酶样蛋白酶体和半胱天冬酶样蛋白酶体的 IC50 分别是1 nM、50-100 nM 和3 μM。

Alkaline tryptase-IN-1 (compound H-13) 是一种靶向碱性类胰蛋白酶的杀虫剂，对禾谷蚜、麦二叉蚜、甘蓝蚜、棉蚜、绣线菊蚜和桃蚜的半致死浓度分别为 8.72、13.77、14.17、12.96 和 12.35 μg mL。

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.

20S Proteasome activator 1 是一种 20S 蛋白酶激活剂，对胰蛋白酶样位点、胰凝乳蛋白酶样位点和半胱天冬酶位点的 IC50 分别为 0.3 μM、0.7 μM 和 1.8 μM。20S Proteasome activator 1 通过在细胞系统中翻译来防止致病性 α-synuclein A53T 突变体积累从而减少疾病发生的概率。20S Proteasome activator 1 可用于研究神经退行性疾病。

Fraxinellone 是从白鲜的根皮中分离出来的一种天然产物，是PD-L1抑制剂，可抑制HIF-1α蛋白质合成。它通过靶向 PD-L1，有用于癌症免疫的潜力。

Nostosin G 是一种独特的线性肽，含有 3 个亚基，4-羟基苯乳酸 (Hpla)，高酪氨酸 (Hty) 和精氨酸。Nostosin G 具有有效的胰蛋白酶抑制特性，其 IC50值为 0.1 μM。

NFF-3 TFA 肽是一种选择性 MMP 底物。NFF-3 TFA 选择性结合 MMP-3和 MMP-10而被水解。NFF-3 TFA 也被胰蛋白酶、肝细胞生长因子激活剂和因子 Xa 裂解。使用 CyDye Cy3 Cy5Q 标记 NFF-3 TFA，可在细胞实验中产生荧光，而检测细胞活性。

Urinary Trypsin Inhibitor Fragment，一种通过蛋白水解生成的尿胰蛋白酶抑制剂片段，能通过有限蛋白水解抑制肿瘤细胞侵袭。

Methoxycarbonyl-D-Nle-Gly-Arg-pNA，这是一种底物，主要用于FIXa (Factors IXa) 和 FXa (Factors Xa)的合成蛋白酶。

Benzenecarboximidamide, hydrochloride, hydrate (1:1:x) (Benzamidine hydrochloride hydrate) 是一种可逆的竞争性胰蛋白酶样丝氨酸蛋白酶 (trypsin-like serine proteases) 抑制剂，对 Tryptase、Trypsin、uPA、Factor Xa、Thrombin 和 tPA 的Ki 值分别为 20、21、97、110、320 和 750 μM。

Pyr-Arg-Thr-Lys-Arg-AMC TFA为AMC肽类化合物，其结构由十肽组成，可经由特异性水解反应由如胰蛋白酶及凝血酶等蛋白酶作用下分解。该肽用于评估蛋白酶活性及酶抑制剂功效的检测。

HA-IN-1（compound 5g）是靶向血凝素（HA）胰蛋白酶切割位点的配体，表现出高亲和力。该化合物能够抑制HA介导的膜融合，并在体内有效降低肺部病毒滴度，展现其作为甲型流感病毒（IAV）抑制剂和抗流感药物的潜力。

Z-Gly-Pro-Arg-AMC hydrochloride是一种合成的多肽，常作为胰蛋白酶和组织蛋白酶K的荧光底物来测定酶的活性，当酶从肽上裂解时会发出荧光。

Calpastatin (184-210), an acetylated synthetic peptide derived from human calpastatin, effectively inhibits the calcium-dependent cysteine proteases, calpain I (µ-calpain) and calpain II (m-calpain), which require micromolar and millimolar calcium concentrations, respectively. Unlike its action on calpains, this 27 amino acid peptide does not inhibit papain (a cysteine protease) or trypsin (a serine protease). Encoded by exon 1B of Ac-calpastatin (184-210), it aligns with a section of inhibitory domain 1, showcasing its specificity and inhibitory function towards calpain enzymes.

4-Nitrophenyl 4-guanidinobenzoate (NPGB) hydrochloride 具有有效抑制精子顶体蛋白 (sperm acrosin) 的功能，并且作为一种胰蛋白酶底物。

23-O-β-D-Glucopyranosyl-20-isoveratramine，一种从荨麻提取的潜在抗过敏剂，含多种抑制剂，如COX-1、COX-2、5-脂氧合酶以及类胰蛋白酶抑制剂和H1 拮抗剂。这些成分对季节性过敏、过敏性鼻炎和其他炎症性疾病具有显著的抑制和预防作用。