heparanase

Heparastatin is an inhibitor of heparanase.

OGT 2115 is an inhibitor of heparanase (IC50 = 0.4 µM), an enzyme that cleaves heparan sulfate into glucuronic acid (GlcUA) and N-acetylglucosamine (GlcNAc). OGT 2115 also showed antiangiogenic properties (IC50=1 μM).

Heparanase 1, Human, is a biocatalyst essential in the novel biocatalysis technology, serving as a key enzyme. Enzyme engineering focuses on improving reaction kinetics, substrate selectivity, and the activity of these enzymes under extreme conditions (e.g., low or high pH). Additionally, introducing stimuli-responsiveness through modifications allows for dynamic control of enzyme activity.

Protein tyrosine phosphatases (PTPs) remove phosphate from tyrosine residues of cellular proteins. Reversible phosphorylation catalyzed by the coordinated actions of protein tyrosine kinases and phosphatases is key to the regulation of the signaling events that control cell growth and proliferation, differentiation, and survival or apoptosis, as well as adhesion and motility. RK-682, a bioactive compound originally isolated from the fermentation of Streptomyces sp. 88-682, is an inhibitor of the PTPs. It inhibits the phosphorylation of CD45 and VHR with IC50 values of 54 and 2 μM, respectively, and arrests cell cycle progress at the G1/S transition. It is also reported to inhibit heparanase (IC50 = 17 μM), an endo-β-D-glucuronidase involved in tumor cell invasion and angiogenesis. RK-682 (calcium salt) is a less soluble version of the free acid.

BIPBIPU is a novel heparanase inhibitor.

HPSE1-IN-1 (compound 16) functions as a selective Heparanase-1 (HPSE1) inhibitor, displaying moderate activity against exo-β-d-glucuronidase (GUSβ) and glucocerebrosidase (GBA) [1].

HPSE1-IN-2 (compound 2) functions as an inhibitor of Heparanase-1 (HPSE1) while concurrently inhibiting exo-β-d-glucuronidase (GUSβ) and glucocerebrosidase (GBA) activities [1].

CV122 is a potent inhibitor of heparanase (heparanase), exhibiting an IC50 of 2.97 µM. This compound inhibits pro-inflammatory cytokines and can be utilized in sepsis research.