KGP94是一种特异性 cathepsin L 抑制剂，IC₅₀ 值为 189 nM，能抑制癌细胞的迁移和侵袭，同时对正常人类细胞的毒性较低 (GI50=26.9µM)，适用于癌症转移研究。

5,5-Dimethyl-2,4-oxazolidinedione is a cathepsin K inhibitor, it's an anticonvulsant.

Cathepsin X-IN-1是一种有效的组织蛋白酶 X 抑制剂，IC50 为 7.13 μM，可降低 PC-3 细胞迁移且具有低细胞毒性。

Cathepsin inhibitor 1 is an inhibitor of Cathepsin (L, L2, S, K, B) with pIC50 of 7.9, 6.7, 6.0, 5.5 and 5.2, respectively.

2-Cyanopyrimidine is a potent and non-selective cysteine protease cathepsin K inhibitor with an IC50 of 170 nM. 2-Cyanopyrimidine is used for osteoporos.

AZD7986 is a second generation reversible covalent, potent and selective DPP1 inhibitor potentially for the treatment of chronic obstructive pulmonary disease (COPD) with predicted human PK properties suitable for once daily human dosing.

CA 074 is an inhibitor of cathepsin B with Ki of 2 - 5 nM.

MDL28170 is a potent, selective inhibitor of calpain and cathepsin B (Ki values are 10 and 25 nM respectively) that does not inhibit trypsin-like serine proteases. MDL28170 rapidly penetrates the blood-brain barrier following systemic administration and displays neuroprotective effects in vivo.

L 006235 is a potent, reversible cathepsin K inhibitor with IC50 of 0.25 nM.

Leupeptin Hemisulfate is a reversible serine/cysteine protease inhibitor, inhibits cathepsins B, H, L, and S, calpain, and trypsin.

LY 3000328 is a highly selective and potent Cathepsin S inhibitor with IC50 of 7.7±5.85 nM and 1.67±1.17 nM for hCat S and mCat S respectively, can be used in treatment for abdominal aortic aneurysm.

Balicatib is a potent and selective inhibitor of cathepsin K ,with 10-100 fold more potent in cell-based enzyme occupancy assays than against cathepsin B, L, and S.

Odanacatib is a potent, selective, and neutral inhibitor of cathepsin K (human/rabbit) with IC50 of 0.2 nM/1 nM, and demonstrated high selectivity versus off-target cathepsin B, L, S.

CA-074 methyl ester是一种特异性的半胱氨酸蛋白酶B抑制剂，具有神经保护、抗癌和抗炎等强效生物活性。

MG-101 is a potent inhibitor of cysteine proteases including calpain I (Ki = 190 nM), calpain II (Ki = 220 nM), cathepsin B (Ki = 150 nM), and cathepsin L (Ki = 500 pM).

E-64（蛋白酶抑制剂E 64）是一种高效的不可逆广谱半胱氨酸蛋白酶抑制剂，对木瓜蛋白酶的IC50为9 nM。

E-64d（E64d）是一种细胞可渗透、不可逆的广谱半胱氨酸蛋白酶抑制剂，对MERS-CoV具有入侵阻断作用。

Atg4B-IN-2是一种有效的Atg4B竞争性抑制剂，其Ki为3.1 μM。它还对PLA2表现出抑制活性，对Atg4B的IC50为11 μM，对PLA2为3.5 μM。Atg4B-IN-2通过自噬增强了抗雄激素耐药前列腺癌分子的抗癌活性。

Furan-2-carboxylic acid, a natural product isolated and purified from the herbs of Hexagonia speciosa with anti-bacterial effect, is also an orally active selective human cathepsin K inhibitor which may have the therapeutic potential for the treatment of diseases characterized by excessive bone loss including osteoporosis.

3-Epiursolic Acid是一种三萜类物质，可以从 Eriobotrya japonica 中分离出来，是竞争性的组织蛋白酶 L (cathepsin L) 抑制剂，IC50 和 Ki 值分别为 6.5 和 19.5 μM，对 cathepsin B 没有明显作用。