heparanase

Heparastatin is an inhibitor of heparanase.

OGT 2115是一种肝素酶(IC50 = 0.4µM)抑制剂，肝素酶是一种将硫酸肝素分解成葡萄糖醛酸(GlcUA)和 n -乙酰氨基葡萄糖(GlcNAc)的酶。同时，OGT 2115也具有抗血管生成性能(IC50=1 μM)。

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) 作为 Heparanase-1 (HPSE1) 的选择性抑制剂，具有针对外切-β-d-葡萄糖醛酸酶 (GUSβ) 和葡萄糖脑苷脂酶 (GBA) 的中等抑制效果。

HPSE1-IN-2（compound 2）作为一种Heparanase-1 (HPSE1) 抑制剂，同时也能抑制外切-β-d-葡萄糖醛酸酶 (GUSβ) 和葡萄糖脑苷脂酶 (GBA) 的活性。

CV122, 一种肝素酶 (heparanase) 抑制剂，具有 2.97 µM 的 IC50 值，能有效抑制促炎细胞因子，适用于败血症的研究。