β-glucuronidase

β-Glucuronidase-IN-3 (Compound 49) is a covalent allosteric inhibitor targeting β-glucuronidase. It exhibits potent inhibitory activity against Escherichia coli β-glucuronidase (EcGUS) with an IC50 of 12.9 nM. The compound exerts its inhibitory effect through reversible covalent modification of cysteine residues (Cys28, Cys443, and Cys197) on EcGUS. It is applicable in research on gut microbiota-related diseases, particularly in reducing the toxic side effects of Irinotecan and non-steroidal anti-inflammatory drugs (NSAIDs).

β-Glucuronidase-responsive conjugate 1 (compound 3) is a well-balanced photosensitizer with photodynamic activity. It effectively inhibits the viability and growth of T-24 cells, with an IC50 of 0.2 μM, and is applicable for bladder cancer research.

β-Glucuronidase-IN-2 is a potent inhibitor of E. coli β-glucuronidase [IC50: 0.24 μM, Ki: 1.09 μM] and exhibits anti-proliferative effects with potential for anti-cancer and anti-inflammatory therapeutic studies.

β-Glucuronidase/hCAII-IN-2 is a potent inhibitor of β-glucuronidase and hCA II, and their IC50 values were 670.7 μM and 21.77 μM, respectively.

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

β-D-Glucuronidase, Bacteria (EC 3.2.1.31) catalyzes the breakdown of complex carbohydrates. It converts conjugated bilirubin into unconjugated bilirubin, facilitating its reabsorption.

Beta-glucuronidase, a critical lysosomal enzyme, is implicated in the breakdown of glucuronate-containing glycosaminoglycans [1].

α-Glucuronidase, Opitutus terrae PB90-1 (EC 3.2.1.139), is a glycosidase that hydrolyzes O- and S-glycosidic compounds. The enzyme specifically acts on two substrates: α-D-glucuronoside and water, producing an alcohol and D-glucuronic acid as its two products.

α-Glucuronidase, Cellvibrio japonicus (EC 3.2.1.139), is a glycosidase responsible for hydrolyzing O- and S-glycoside compounds. This enzyme acts on α-D-glucuronosides and water, producing alcohol and D-glucuronic acid as its two resultant products.

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.

2,2'-Dihydroxy chalcone is a potent inhibitor of β-glucuronidase (IC50=1.6±0.2 μM) and lysozyme (IC50=1.4±0.2 μM) release from rat neutrophils stimulated with fMLP/CB.2,2'-Dihydroxy chalcone has inhibitory activity against Escherichia coli, Shigella fowleri, Staphylococcus albicans and Staphylococcus aureus.

D-Saccharic acid 1,4-lactone hydrate is a potent β-glucuronidase inhibitor (IC50=48.4 μM) that possesses anticarcinogenic, detoxifying, and antioxidant properties[1][2].

2-(4-chlorophenyl)quinazolin-4-ol is an effective inhibitor of β-glucuronidase (IC₅₀ = 39.8 µM), and can be used in the study of glucuronidase-related diseases.

Ganoderenic acid A has a potent hepatoprotective, and cytotoxic effects, it shows inhibitory activity on human aldose reductase in vitro.

EHT 1610 (EHT 5372) is a potent inhibitor of DYRK, with an IC50 of 0.36 nM and 0.59 nM for DYRK1A and DYRK1B, respectively. EHT 1610 has an inhibitory effect on leukemia, regulating cell cycle and inducing cell apoptosis.

GSK-626616 is a potent and orally bioavailable DYRK3 inhibitor (IC50: 0.7 nM). It inhibits other members of the DYRK family with similar potency. GSK-626616 is a potential therapy for the treatment of anemia.

hCAII-IN-4 (Compound 12j) is a potent inhibitor of human carbonic anhydrase II (hCA II) with an IC50 of 7.78 μM, and also inhibits β-glucuronidase with an IC50 of 773.9 μM [1].

DMAT (Casein kinase II Inhibitor) is a potent and specific inhibitor of CK2(IC50 value of 130 nM).

Kushenol X exhibits inhibitory activity against Sodium-dependent glucose cotransporter 2(SGLT2).

2'-Hydroxydaidzein is an isoflavonoid phytonutrient found in plant species, when a natural compound. 2'-Hydroxydaidzein has antioxidant activity, driven mainly by o-hydrogen bond dissociation enthalpy (BDE) and hydrogen atom transfer (HAT) mechanisms. 2'-Hydroxydaidzein inhibits chemical mediators in inflammatory cells and may be of value in the treatment and prevention of inflammatory diseases associated with excessive chemical mediator production. It may have a role in the treatment and prevention of central and peripheral inflammatory diseases associated with excessive chemical mediator production. 2'-Hydroxydaidzein inhibited the release of neutrophils and formyl-Met-Leu-Phe/cytochalasin B (fMLP/CB) in rats, with IC(50) values of 2.8+/-0.1 and 5.9+/-1.4 microM, respectively.

6-Chloro-3-indolyl-β-D-Glucuronide (cyclohexylammonium salt) is a chromogenic substrate for β-glucuronidase and can be utilized in the histochemical analysis of β-glucuronidase activity.

(+)-Guaiacin, isolated from the bark of Machilus wangchiana Chun, demonstrates potent in vitro inhibition of β-glucuronidase release in rat polymorphonuclear leukocytes (PMNs) induced by platelet-activating factor (PAF).

EcGUS-IN-1 (Compound E-9) is a non-competitive inhibitor of β-glucuronidase, featuring an IC50 value of 2.68 μM and a Ki value of 1.64 μM. This compound effectively mitigates gastrointestinal adverse events (GIAE) associated with Escherichia coli infections by inhibiting the activity of E. coli β-glucuronidase.

Saccharic acid serves as a competitive inhibitor of β-glucuronidase. It significantly slows down the hydrolysis of "l-ortho-hydroxyphenylazo-2-naph-thol" glucuronide in frozen-thawed mouse kidney slices, yet it does not impact liver regeneration following injury or the growth of infant mice.