2. Metabolic Enzyme/Protease Immunology/Inflammation
  3. Phosphatase PD-1/PD-L1
  4. LYP-IN-3

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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LYP-IN-3

LYP-IN-3 Chemical Structure

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
5 mg In-stock
10 mg In-stock
25 mg In-stock
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Based on 1 publication(s) in Google Scholar

LYP-IN-3 Related Antibodies

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Description

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[1].

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.

LYP-IN-3 Related Antibodies

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.
Molecular Weight

589.66

Formula

C35H27NO6S
Appearance

Solid

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6959 mL 8.4795 mL 16.9589 mL
5 mM 0.3392 mL 1.6959 mL 3.3918 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

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.

  • 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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
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 1.6959 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 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

LYP-IN-3PhosphatasePD-1/PD-L1PD-1/Programmed death-ligand 1LYPCancer ImmunotherapyPD-1/PD-L1 BlockadeTCR Signaling PathwayColorectal CancerCRCInhibitorinhibitorinhibit

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