CAS NO: | 329317-98-8 |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 608.6 |
Cas No. | 329317-98-8 |
Formula | C26H26F6N2O4S2 |
Synonyms | Protein Tyrosine Phosphatase Inhibitor IV |
Solubility | ≤25mg/ml in ethanol;25mg/ml in DMSO;30mg/ml in dimethyl formamide |
Chemical Name | N,N'-[1,4-phenylenebis[(1-methylethylidene)-4,1-phenylene]]bis[1,1,1-trifluoro-methanesulfonamide |
Canonical SMILES | O=S(NC1=CC=C(C(C)(C)C2=CC=C(C(C)(C)C3=CC=C(NS(=O)(C(F)(F)F)=O)C=C3)C=C2)C=C1)(C(F)(F)F)=O |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
IC50: 1.8, 2.5, 8.4, 13, 20, 6.4, and 6.7 μM for SHP-2, PTP1B, PTP-ε, PTP-Meg-2, PTP-σ, PTP-β, and PTP-μ, respectively
PTP Inhibitor IV is a protein tyrosine phosphatases (PTPs) inhibitor.
PTPs are reported to be important in the regulation of various signal transduction processes. Enzymes of this class are considered as potential therapeutic targets in the treatment of various diseases including inflammation, diabetes, as well as cancer. However, previously identified PTP inhibitors are peptide-based containing a highly charged component, which usually lack membrane permeability resulting in their limited utility in the inhibition of intracellular phosphatases.
In vitro: PTP inhibitor IV was identified as an uncharged, 1,4-di-substituted, phenyl-linked bis-trifluoromethylsulfonamido phosphate mimetic acting as a competitive, reversible, and active-site directed inhibitor. It was noticed that PTP inhibitor IV showed greatly increased potency not only on PTP1B but also on the phosphatases SHP-2 and Mu. Moreover, the interaction of the second SO2CF3 moiety in PTP inhibitor IV with conserved Arg residue of PTP might explain the increased inhibitory potency towards other PTPs in addition to PTP1B [1].
In vivo: Up to now, there is no animal in vivo data reported.
Clinical trial: So far, no clinical study has been conducted.
Reference:
[1] Huang, P. ,Ramphal, J.,Wei, J., et al. Structure-based design and discovery of novel inhibitors of protein tyrosine phosphatases. Bioor.Med.Chem. 11, 1835-1849 (2003).