PTPS

DiFMUP (6,8-Difluoro-4-methylumbelliferyl phosphate) 是一种荧光底物，抑制蛋白酪氨酸磷酸酶（PTPs），可用于检测苏氨酸磷酸酶的活性。

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.

LYP-IN-1 is a powerful LYP inhibitor that demonstrates high potency, selectivity, and specificity, with a Ki of 110 nM and an IC 50 of 0.259 μM. Beyond its primary target, LYP-IN-1 also exhibits selectivity towards a wide range of PTPs, including SHP1 (IC 50 = 5 μM) and SHP2 (IC 50 = 2.5 μM). Additionally, LYP-IN-1 demonstrates remarkable efficacy in T- and mast cells, making it a valuable tool for investigating autoimmune disorders.

3,5-Difluoro-L-tyrosine is a functional and tyrosinase-resistant mimic of tyrosine, commonly utilized for evaluating the substrate specificity of protein tyrosine phosphatases (PTPs).

MLS-0437605 is a potent and selective inhibitor of dual-specificity phosphatase 3 (DUSP3), with an IC50 of 3.7 μM. It exhibits higher selectivity towards DUSP3 in comparison to DUSP22 and other protein tyrosine phosphatases (PTPs).

NAZ2329 是受体型蛋白质酪氨酸磷酸酶 (RPTPs) R5 亚家族的一个细胞可渗透抑制剂，与其他 PTPs 相比，其变构且能够优先抑制 PTPRZ (hPTPRZ1 的IC50= 7.5 μM) 和PTPRG (hPTPRGIC50= 4.8 μM)。NAZ2329 能够与PTPRZ 的 D1结构域结合，与PTPRZ 整个 (D1 + D2) 片段相比，其能够更有效地抑制 PTPRZ1-D1片段 (IC50: 1.1 μM)。NAZ2329 能够抑制胶质母细胞瘤细胞的肿瘤生长，并表现出抑制干细胞样特性。

PTPσ Inhibitor, ISP 结合并抑制重组人PTPσ的信号传导，具有穿透细胞膜的能力，有助于缓解CSPG介导的脊髓损伤模型中轴突的生长抑制。该抑制剂能增强LPC引起的脊髓脱髓鞘损伤的髓鞘再生，并在MS动物模型中促进OPC的迁移、分化、髓鞘形成及功能恢复。