LYP-IN-3
Based on 1 Customer Validation
LYP-IN-3 is a selective, orally active and reversible lymphoid-tyrosine phosphatase (LYP) inhibitor (IC50 = 2.55 μM, Ki = 0.93 μM). D34 exhibits high selectivity of PTP1B, PTPN12, PTPN5 and SSH2. LYP-IN-3 regulates the T-cell receptor (TCR) signaling by specifically inhibiting LYP. LYP-IN-3 does not significantly inhibit MC38 cell viability; its anti-tumor effect stems from immune regulation. LYP-IN-3 can significantly upregulate PD-L1 or PD-1 expression in different immune cells. LYP-IN-3 facilitates T-cell infiltration and enhances T-cell functions. LYP-IN-3 synergizes with PD-L1 blockade can significantly improve colorectal tumor regression. LYP-IN-3 can be used for the study of colorectal cancer.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.80%
- No. CAS: 3052262-64-0
- Fòrmula: C35H27NO6S
- Peso molecular:589.66
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Almacenamiento: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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
Ki: 0.93 μM (Lymphoid-tyrosine phosphatase, LYP)[1]
LYP-IN-3 (Compound D34) (15 μM, 1 h) increases levels of phosphorylation of LCK and ERK in Jurkat T cells, stimulating TCR signaling through specific inhibition of LYP[1].
LYP-IN-3 (0-4 μM, 72 h) has no significant inhibitory effect on MC38 cell viability[1].
D34 (10 μM, 20 μM, 48 h) can upregulate PD-L1 expression of MC38 cells in a dose-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Jurkat T cells
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Concentration:15 μM
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Incubation Time:1 h
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Result:Led to increased levels of phosphorylation of LCK and ERK.
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Cell Line:MC38 cells
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Concentration:0 μM, 0.5 μM, 1 μM, 2 μM, 4 μM
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Incubation Time:72 h
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Result:Had no significant inhibitory effect on the survival rate of MC38 cells.
LYP-IN-3 (50 mg/kg, oral gavage, twice daily for 14 days) combines with PD-L1 blockade, significantly improves colorectal tumor regression[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:1.0 × 106 MC38 cells were injected subcutaneously into the right armpits of C57BL/6J mice to establish the MC38 cell syngeneic mouse tumor model[1].
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Dosage:50 mg/kg
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Administration:Oral gavage, twice a day for 14 days
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Result:Significantly suppressed tumor growth in vivo with TGI = 65%.
Significantly increased the proportion of lymphocytes (CD45+) in the tumor microenvironment.
Increased the proportion of CD4+ T cells and CD8+ T cells in the tumor microenvironment with increased expression of Ki67.
Significantly upregulated the tumor infiltration of CD8+ T cells. Increased the proportion of M1 TAMs and inhibited the M2 polarization of TAMs.
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Animal Model:1.0 × 106 MC38 cells were injected subcutaneously into the right armpits of C57BL/6J mice to establish the MC38 cell syngeneic mouse tumor model[1].
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Dosage:PD-L1: 4 mg/kg
LYP-IN-3: 50 mg/kg -
Administration:PD-L1: Once every two days, Intraperitoneal injections
LYP-IN-3: Twice a day, Oral gavage -
Result:The combined use of LYP-IN-3 with PD-L1 blockade showed stronger tumor regression.
Chemical Information
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No. CAS 3052262-64-0
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Appearance Solid
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Peso molecular 589.66
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Fòrmula C35H27NO6S
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Color White to off-white
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SMILES
O=C(C1=CC2=CC(N(CC3=CC=C(OCC4=CC=CC=C4)C=C3)S(=O)(C5=CC=C(C6=CC=CC=C6)C=C5)=O)=CC=C2O1)O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 100 mg/mL (169.59 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)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (4.24 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (278 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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 |
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| DMSO | 1 mM | 1.6959 mL | 8.4795 mL | 16.9589 mL | 42.3973 mL |
| 5 mM | 0.3392 mL | 1.6959 mL | 3.3918 mL | 8.4795 mL | |
| 10 mM | 0.1696 mL | 0.8479 mL | 1.6959 mL | 4.2397 mL | |
| 15 mM | 0.1131 mL | 0.5653 mL | 1.1306 mL | 2.8265 mL | |
| 20 mM | 0.0848 mL | 0.4240 mL | 0.8479 mL | 2.1199 mL | |
| 25 mM | 0.0678 mL | 0.3392 mL | 0.6784 mL | 1.6959 mL | |
| 30 mM | 0.0565 mL | 0.2826 mL | 0.5653 mL | 1.4132 mL | |
| 40 mM | 0.0424 mL | 0.2120 mL | 0.4240 mL | 1.0599 mL | |
| 50 mM | 0.0339 mL | 0.1696 mL | 0.3392 mL | 0.8479 mL | |
| 60 mM | 0.0283 mL | 0.1413 mL | 0.2826 mL | 0.7066 mL | |
| 80 mM | 0.0212 mL | 0.1060 mL | 0.2120 mL | 0.5300 mL | |
| 100 mM | 0.0170 mL | 0.0848 mL | 0.1696 mL | 0.4240 mL |
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