Bortezomib是一种可逆性和选择性的蛋白酶体 (proteasome) 抑制剂，通过靶向苏氨酸残基有效抑制 20S 蛋白酶体 (Ki=0.6 nM)。Bortezomib 主要用于多发性骨髓瘤和其他血液癌症的治疗研究。

MLN9708 is the prodrug of MLN2238 which is an inhibitor of the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with IC50 and Ki of 3.4 nM, 0.93 nM, respectively.

Ixazomib（MLN2238）是一种选择性、强效和可逆的蛋白酶体抑制剂，靶向20S蛋白酶体的胰凝乳蛋白酶样蛋白水解（β5）位点，IC50为3.4 nM，Ki为0.93 nM。

ONX 0912 is an inhibitor of proteasome that targets the chymotrypsin-like activity of the 20S proteasome subunits β5 (IC50 = 36 nM) and LMP7 (IC50 = 82 nM).

Delanzomib is an orally active inhibitor of the chymotrypsin-like activity of proteasome with IC50 of 3.8 nM, with only marginal inhibition of the tryptic and peptidylglutamyl activities of the proteosome.

Celastrol (Tripterine; Tripterin) 是一种蛋白酶体抑制剂，以 IC50 为 2.5 μM 强效且优先抑制纯化 20S 蛋白酶体的胰凝乳蛋白酶样活性。

PI-1840 是一种有效的选择性组织蛋白酶 L (CT-L) 抑制剂，IC50 为 27 nM。PI-1840 抑制细胞增殖，阻滞细胞周期在 G2/M 期，诱导凋亡和自噬。

Epoxomicin is a potent anti-tumor agent isolated from Actinomycetes that is used as a selective and irreversible inhibitor of the 20S proteasome.