Art. -Nr.: HY-155847

LYP-IN-3

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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.

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Reinheit: 99.80%
CAS. Nr.: 3052262-64-0
Formel: C₃₅H₂₇NO₆S
Molecular Weight:589.66

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

LYP-IN-3 Chemical Structure

CAS. Nr.: 3052262-64-0

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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.

Western Blot Analysis^[1]

Cell Line:

Jurkat T cells
Concentration:

15 μM
Incubation Time:

1 h
Result:

Led to increased levels of phosphorylation of LCK and ERK.

Cell Viability Assay^[1]

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) significantly inhibited MC38 tumor growth by enhancing anti-tumor immunity, and its mechanism of action involved T cell activation and regulation of macrophage polarization, rather than direct cytotoxicity^[1].
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. Nr. 3052262-64-0
Appearance Solid
Molecular Weight 589.66
Formel 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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.6959 mL

8.4795 mL

16.9589 mL

5 mM

0.3392 mL

1.6959 mL

3.3918 mL

10 mM

0.1696 mL

0.8479 mL

1.6959 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: 2.5 mg/mL (4.24 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL. If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during 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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Liang X, et al. Discovery of benzofuran-2-carboxylic acid derivatives as lymphoid tyrosine phosphatase (LYP) inhibitors for cancer immunotherapy. Eur J Med Chem. 2023 Oct 5;258:115599. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

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LYP-IN-3

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Small Molecule Immuno-Oncology Compound Library

Orally Active Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Phosphatase Inhibitor Library

Anti-Obesity Compound Library

Anti-Colorectal Cancer Compound Library

Metabolic Enzyme Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Extracellular Vesicles (EVs) Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

LYP-IN-3

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Small Molecule Immuno-Oncology Compound Library

Orally Active Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Phosphatase Inhibitor Library

Anti-Obesity Compound Library

Anti-Colorectal Cancer Compound Library

Metabolic Enzyme Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Extracellular Vesicles (EVs) Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

LYP-IN-3 Related Classifications

HY-155847 Related Classifications