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Art. -Nr.: HY-179648

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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.

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CAS. Nr.: 1240857-57-1
Formel: C₁₉H₁₇FN₂O₃
Molecular Weight:340.35

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (269 KB)

CD28-IN-2 Chemical Structure

CAS. Nr.: 1240857-57-1

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- In Vitro
- Parmacokinetics
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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.

ELISA Assay^[1]

Cell Line:

A 3D coculture model comprising IFN-γ-primed A549 tumor spheroids and human PBMCs.
Concentration:

10 μM, 25 μM, 50 μM
Incubation Time:

48 h
Result:

Resulted in concentration-dependent suppression of Tcell activation, indicating effective inhibition of CD28-mediated costimulation.

Parmacokinetics

Species	Dose	Route	C_max	AUC_0-t	T_1/2	T_max	CL	V_d
Mice^[1]	2 mg/kg	i.v.	4,440 ng/mL	10,392 ng·h/mL	1.62 h	/	3.21 mL/min/kg	0.45 L/kg
Mice^[1]	10 mg/kg	p.o.	3,024 ng/mL	9,401 ng·h/mL	2.55 h	1.12 h	/	/

Chemical Information

CAS. Nr. 1240857-57-1
Molecular Weight 340.35
Formel C₁₉H₁₇FN₂O₃
SMILES

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

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (269 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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