CD28-IN-2
CD28-IN-2 is a selective CD28-B7 interaction (IC50: 22.4 μM) inhibitor that binds directly to CD28, with a Kd value of 24.1 μM. CD28-IN-2 inhibits CD28-driven immune activation and blocks T cell costimulation. CD28-IN-2 can be used for the study of antitumor immunity and immune-related disorders.
For research use only. We do not sell to patients.
- CAS No.: 1240857-57-1
- Formula: C19H17FN2O3
- Molecular Weight:340.35
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
In Vitro
CD28-IN-2 (5MS-5) (10-50 μM; 48 hours) effectively inhibits CD28-dependent cytokine release and T cell activation markers (such as IFN-γ, IL-2,and soluble CD69 (sCD69)) in a 3D coculture model comprising IFN-γ-primed A549 tumor spheroids and human PBMCs[1].
In CD28-expressing Jurkat T cells containing a TCR/CD3-CD28-responsive luciferase reporter are cocultured with Raji antigen-presenting cells, CD28-IN-2 exhibits dose-dependent inhibition of CD28-mediated luminescence, with an IC50 of 10.3 μM[1].
CD28-IN-2 shows a weak inhibition of the hERG potassium channel (IC50 > 50 μM). CD28-IN-2 against major cytochrome P450 isoforms revealed minimal inhibition at 10 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:A 3D coculture model comprising IFN-γ-primed A549 tumor spheroids and human PBMCs.
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Concentration:10 μM, 25 μM, 50 μM
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Incubation Time:48 h
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Result:Resulted in concentration-dependent suppression of Tcell activation, indicating effective inhibition of CD28-mediated costimulation.
Parmacokinetics
Chemical Information
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CAS No. 1240857-57-1
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Molecular Weight 340.35
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Formula C19H17FN2O3
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SMILES
COC1=CC=C(CC(OCC2=CC=C(C=C2)N3C=CC=N3)=O)C=C1F
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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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.
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Research Protocol for Cancer Immunology
Cancer immunology studies how the immune system recognizes, suppresses, edits, or fails to eliminate malignant cells through tumor antigen release, antigen presentation, T-cell priming, immune trafficking, tumor-cell killing, and feedback inhibition in the tumor microenvironment. The cancer-immunity cycle links tumor antigenicity, dendritic-cell priming, CD8+ T-cell infiltration, cytotoxic function, and immune-checkpoint regulation to tumor rejection or immune escape. Immune-checkpoint pathways such as PD-1/PD-L1 and CTLA-4 suppress antitumor T-cell activity and can be therapeutically blocked, but many tumors remain resistant because of poor antigen presentation, weak T-cell infiltration, suppressive myeloid cells, regulatory T cells, and tumor-intrinsic immune-exclusion programs. Unresolved questions include which immune-cell states predict response, how tumor-intrinsic pathways exclude immune cells, how myeloid suppression limits checkpoint blockade, and which combination strategies
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)