PTPRO-IN-1
Based on 1 Customer Validation
PTPRO-IN-1 is a selective, orally active PTPRO inhibitor with an IC50 of 0.16 μM. PTPRO-IN-1 exhibits IC50 values of 2.4 μM, 2.33 μM and 2.13 μM against PTPN22, PTP1B and PTPRT, respectively, and shows almost no inhibitory activity against STEP/SSH2. PTPRO-IN-1 inhibits the TLR4/NF-κB signaling pathway in macrophages, ameliorates colonic pathological conditions and suppresses the secretion of pro-inflammatory cytokines by T cells. PTPRO-IN-1 can be used for the research of inflammatory bowel disease.
For research use only. We do not sell to patients.
- Formula: C36H24ClNO6S
- Molecular Weight:634.10
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
TLR4 |
IL-6 |
In Vitro
PTPRO-IN-1 (Compound 30k) (5 μM; 30 h) dose-dependently inhibits LPS (HY-D1056)-induced p-p65 expression and IL-6 secretion, as well as upregulation of TLR4 and phosphorylation of IKKα/β, in murine RAW264.7 and human THP-1 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LPS-stimulated Raw 264.7 cells and THP-1-derived macrophages
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Concentration:5 μM
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Incubation Time:24 hours, followed by 1 μg/mL LPS stimulation for 4 hours
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Result:Dose-dependently inhibited LPS-induced p-p65 and IL-6 secretion.
Inhibited TLR4 upregulation and phosphorylation of IKKα/β.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:male C57BL/6J mice (6-8 weeks
old)[1] -
Dosage:20 mg/kg
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Administration:i.g.; once daily for 10 days
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Result:Significantly reversed intestinal shortening and alleviated histological inflammation.
Significantly down-regulated the secretion of IFN-γ and IL-2 in CD4⁺/CD8⁺ T cells.
Chemical Information
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Appearance Solid
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Molecular Weight 634.10
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Formula C36H24ClNO6S
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Color White to off-white
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SMILES
OC1=CC=C(C#CC2=CC=C(C=C2)N(S(C3=CC=C4OC(C(O)=O)=CC4=C3)(=O)=O)CC5=CC=C(C=C5)C6=CC(Cl)=CC=C6)C=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 50 mg/mL (78.85 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.5770 mL | 7.8852 mL | 15.7704 mL | 39.4260 mL |
| 5 mM | 0.3154 mL | 1.5770 mL | 3.1541 mL | 7.8852 mL | |
| 10 mM | 0.1577 mL | 0.7885 mL | 1.5770 mL | 3.9426 mL | |
| 15 mM | 0.1051 mL | 0.5257 mL | 1.0514 mL | 2.6284 mL | |
| 20 mM | 0.0789 mL | 0.3943 mL | 0.7885 mL | 1.9713 mL | |
| 25 mM | 0.0631 mL | 0.3154 mL | 0.6308 mL | 1.5770 mL | |
| 30 mM | 0.0526 mL | 0.2628 mL | 0.5257 mL | 1.3142 mL | |
| 40 mM | 0.0394 mL | 0.1971 mL | 0.3943 mL | 0.9856 mL | |
| 50 mM | 0.0315 mL | 0.1577 mL | 0.3154 mL | 0.7885 mL | |
| 60 mM | 0.0263 mL | 0.1314 mL | 0.2628 mL | 0.6571 mL |
PTPRO-IN-1 Related Classifications
HY-183573 Related Classifications
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