2. Immunology/Inflammation
  3. PD-1/PD-L1
  4. GJ19

GJ19 is a PD-L1 inhibitor with an IC50 of 32.06 nM. GJ19 can effectively bind to human/murine PD-L1 protein with KD values of 171 and 290 nM, respectively. GJ19 concentration-dependently promotes HepG2 cell mortality in a co-culture model of HepG2/hPD-L1 and Jurkat T/hPD-1 cells. GJ19 effectively suppresses tumor growth in a B16-F10 melanoma mouse model. GJ19 can be used for the study of tumor immunotherapy.

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GJ19

GJ19 Chemical Structure

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GJ19 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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Description

GJ19 is a PD-L1 inhibitor with an IC50 of 32.06 nM. GJ19 can effectively bind to human/murine PD-L1 protein with KD values of 171 and 290 nM, respectively. GJ19 concentration-dependently promotes HepG2 cell mortality in a co-culture model of HepG2/hPD-L1 and Jurkat T/hPD-1 cells. GJ19 effectively suppresses tumor growth in a B16-F10 melanoma mouse model. GJ19 can be used for the study of tumor immunotherapy[1].

In Vitro

GJ19 (48 h) demonstrates the highest PD-L1 inhibitory effects with an IC50 of 32.06 nM in the HTRF assay, which is better than the positive control BMS-202 (HY-19745) (IC50 = 62.1 nM)[1].

GJ19 (0.1-10 μM) binds to human/murine PD-L1 protein nicely, with KD values of 171 and 290 nM, respectively[1].

GJ19 (48 h) exhibits no/little cytotoxicity against the tested tumor cells (murine/human melanoma cell lines B16-F10/A375 human liver cancer cell line HepG2, and human breast cells MDA-MB-23l and Jurkat T cells) and exerts toxicity only upon co-culture with T cells[1].

GJ19 (12.3-1000 nM, 24 h) dose-dependently and significantly increases the mortality of HepG2 cells in the HepG2/Jurkat T cell co-culture system, and the mortality rate of HepG2 cells is higher than that of the positive control BMS-202 at a concentration of 1000 nM[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

GJ19 Related Antibodies
In Vivo

GJ19 (5-15 mg/kg, i.p.) exhibits potent antitumor efficacy with a TGI of 56.8% at the dose of 15 mg/kg in a B16-F10 melanoma mouse model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 6-8 weeks male C57BL/6 mice were inoculated with B16-F10 cells into the right armpit (2.5×105)[1]
Dosage: 5, 15 mg/kg
Administration: i.p.
Result: Reduced both the tumor weights without affecting the body weight of mice.
Increased the percentages of CD3+ CD4+ cells (helper T cells) and CD3+ CD8+ cells (activated cytotoxic T cells) in melanoma tumors.
Decreased PD-L1 levels in the tumor.
Showed no abnormalities in the weight of major organs (heart, liver, and kidney).
Molecular Weight

628.11

Formula

C32H31ClFNO7S
Appearance

Solid

Color

White to off-white

SMILES

C[C@H](O)[C@H](C(O)=O)NCC1=CC(Cl)=C(OCC2=C(C)C(C3=CC=CC=C3)=CC=C2)C=C1OCC4=CC=C(S(=O)(F)=O)C=C4
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 (159.21 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 1.5921 mL 7.9604 mL 15.9208 mL
5 mM 0.3184 mL 1.5921 mL 3.1842 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
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
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 (3.98 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (3.98 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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 1.5921 mL 7.9604 mL 15.9208 mL 39.8019 mL
5 mM 0.3184 mL 1.5921 mL 3.1842 mL 7.9604 mL
10 mM 0.1592 mL 0.7960 mL 1.5921 mL 3.9802 mL
15 mM 0.1061 mL 0.5307 mL 1.0614 mL 2.6535 mL
20 mM 0.0796 mL 0.3980 mL 0.7960 mL 1.9901 mL
25 mM 0.0637 mL 0.3184 mL 0.6368 mL 1.5921 mL
30 mM 0.0531 mL 0.2653 mL 0.5307 mL 1.3267 mL
40 mM 0.0398 mL 0.1990 mL 0.3980 mL 0.9950 mL
50 mM 0.0318 mL 0.1592 mL 0.3184 mL 0.7960 mL
60 mM 0.0265 mL 0.1327 mL 0.2653 mL 0.6634 mL
80 mM 0.0199 mL 0.0995 mL 0.1990 mL 0.4975 mL
100 mM 0.0159 mL 0.0796 mL 0.1592 mL 0.3980 mL
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GJ19 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:

GJ19GJ 19GJ-19PD-1/PD-L1PD-1/Programmed death-ligand 1HepG2Jurkat TPD-L1cancerInhibitorinhibitorinhibit

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