β-Glucuronidase-IN-1 is an E. coli β-glucuronidase (β-glucuronidase) inhibitor with a potent, selective, non-competitive, and orally active IC50 and Ki value of 283 nM and 164 nM, respectively, against E. coli β-glucuronidase.

β-Glucuronidase/hCAII-IN-2 (Compound 12e) is a compound that effectively inhibits both β-glucuronidase and human Carbonic Anhydrase II (hCA II), exhibiting IC50 values of 440.1 μM and 4.91 μM, respectively [1].

β-Glucuronide-NB-bis[N(Me)-methyl ester]-MMAE (compound 20), an auristatins-glucuronide conjugate, exhibits in vitro antiproliferative effects on cancer cells, both β-glucuronidase pretreated and untreated, with an IC50 range of 5.7 nM to 9.7 nM. Demonstrating powerful antitumor efficacy in an HCT-116 xenograft mouse model, this compound does not induce side effects [1].

hCAII-IN-4 (Compound 12j) is a potent inhibitor of human carbonic anhydrase II (hCA II), exhibiting an inhibitory concentration (IC50) of 7.78 μM. Additionally, it demonstrates inhibition of β-glucuronidase, presenting an IC50 value of 773.9 μM [1].