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 Chemical Structure

GJ19 Chemical Structure

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GJ19 Related Antibodies

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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 (5-15mg/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
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
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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GJ19 Related Classifications

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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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