CD28-IN-2 

CD28-IN-2 is a selective CD28-B7 interaction (IC₅₀: 22.4 μM) inhibitor that binds directly to CD28, with a K_d 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^[1].

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.

340.35

C₁₉H₁₇FN₂O₃

1240857-57-1

COC1=CC=C(CC(OCC2=CC=C(C=C2)N3C=CC=N3)=O)C=C1F

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• [1]. Upadhyay S, et al. Discovery of CD28-Targeted Small Molecule Inhibitors of T Cell Co-Stimulation Using Affinity Selection-Mass Spectrometry (AS-MS) and Ex Vivo Validation. J Med Chem. 2025;68(23):25112-25125.  [Content Brief]