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.
For research use only. We do not sell to patients.
- Purity : 99.80%
- CAS No.: 3052262-64-0
- Formula: C35H27NO6S
- Molecular Weight:589.66
-
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]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Protocols
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
Description
IC50 & Target
Ki: 0.93 μM (Lymphoid-tyrosine phosphatase, LYP)[1]
In Vitro
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. Further protocols information, click here.
-
Cell Line:Jurkat T cells
-
Concentration:15 μM
-
Incubation Time:1 h
-
Result:Led to increased levels of phosphorylation of LCK and ERK.
-
Cell Line:MC38 cells
-
Concentration:0 μM, 0.5 μM, 1 μM, 2 μM, 4 μM
-
Incubation Time:72 h
-
Result:Had no significant inhibitory effect on the survival rate of MC38 cells.
In Vivo
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.
-
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].
-
Dosage:50 mg/kg
-
Administration:Oral gavage, twice a day for 14 days
-
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.
-
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].
-
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
-
CAS No. 3052262-64-0
-
Appearance Solid
-
Molecular Weight 589.66
-
Formula C35H27NO6S
-
Color White to off-white
-
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
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
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 : 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)
In Vivo:
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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%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.
Protocols
-
RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
-
Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
-
Mammalian live/dead viability and cytotoxicity staining
Live/dead viability and cytotoxicity staining assays are based on the simultaneous detection of intracellular esterase activity in metabolically active (viable) cells and membrane integrity loss in non-viable cells. In commonly used dual-staining approaches, membrane-permeant fluorogenic substrates are converted by intracellular esterases into fluorescent products in live cells, while impermeant DNA-binding dyes selectively enter cells with compromised plasma membranes and label nucleic acids in dead or dying cells, enabling discrimination between viable and non-viable populations by fluorescence microscopy or flow cytometry.
-
CCK-8/WST-8 Cell Proliferation Assay
The CCK-8/WST-8 assay is based on the reduction of the water-soluble tetrazolium salt WST-8 to a water-soluble formazan product by cellular dehydrogenases in metabolically active cells, where the generated formazan amount is proportional to the number of living cells and is quantified by measuring absorbance in the visible range, providing a colorimetric readout for cell viability and proliferation assessment. This class of tetrazolium-based assays improves upon earlier MTT-based systems by producing a water-soluble formazan, eliminating the need for organic solubilization steps and enabling direct spectrophotometric measurement in culture medium.
-
MTT Cell Proliferation Assay
The MTT assay is a colorimetric endpoint assay for estimating viable cell number, cell growth, cytotoxicity, or cell activation in cultured mammalian cells. Living cells reduce the yellow tetrazolium salt MTT into purple/blue formazan, while dead cells do not generate the same signal; the resulting color can be quantified with a multiwell spectrophotometer. MTT reduction is commonly interpreted as a readout of metabolic activity that often correlates with viable cell number, but it should not be treated as a direct cell-counting method unless the assay is optimized for the cell type and experimental condition. Studies show that MTT reduction can involve mitochondrial and non-mitochondrial reducing systems, and formazan may accumulate in intracellular lipid droplets rather than simply marking mitochondria.
-
Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Purity & Documentation
-
Data Sheet (278 KB)
-
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)
-
Handling Instructions (2659 KB)
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 | 1.6959 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 |
LYP-IN-3 Related Classifications
HY-155847 Related Classifications
Powered by Bioz