PTP Inhibitor IV (Synonyms: Protein Tyrosine Phosphatase Inhibitor IV) |
| رقم الكتالوجGC15969 |
PTP inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 329317-98-8
Sample solution is provided at 25 µL, 10mM.
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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).
| Cas No. | 329317-98-8 | SDF | |
| المرادفات | Protein Tyrosine Phosphatase Inhibitor IV | ||
| 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 | ||
| Formula | C26H26F6N2O4S2 | M.Wt | 608.6 |
| الذوبان | ≤25mg/ml in ethanol;25mg/ml in DMSO;30mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.6431 mL | 8.2156 mL | 16.4312 mL |
| 5 mM | 0.3286 mL | 1.6431 mL | 3.2862 mL |
| 10 mM | 0.1643 mL | 0.8216 mL | 1.6431 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 40 reference(s) in Google Scholar.)
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