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Chemical Structure| 39544-74-6 Chemical Structure| 39544-74-6

Structure of Benzotript
CAS No.: 39544-74-6

Chemical Structure| 39544-74-6

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Synonyms: Benzotriptum

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Product Citations

Faisal Aziz ; Kanamata Reddy ; Virneliz Fernandez Vega ; Raja Dey ; Katherine A. Hicks ; Sumitha Rao , et al.

Abstract: The suppressor of T cell receptor signaling (Sts) proteins are negative regulators of immune signaling. Genetic inactivation of these proteins leads to significant resistance to infection. From a 590,000 compound high-throughput screen, we identified the 2-(1H)-quinolinone derivative, , as a putative inhibitor of Sts activity. , and a small library of derivatives, are competitive, selective inhibitors of Sts-1 with IC50 values from low to submicromolar. SAR analysis indicates that the , the acid, and the moieties are all essential for activity. A crystal structure confirmed the SAR and reveals key interactions between this class of compound and the . Although has poor cell permeability, we demonstrated that a liposomal preparation can inactivate the activity of Sts-1 in cells. These studies demonstrate that Sts-1 enzyme activity can be pharmacologically inactivated and provide foundational tools and insights for the development of immune-enhancing therapies that target the Sts proteins.

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Product Details of Benzotript

CAS No. :39544-74-6
Formula : C18H15ClN2O3
M.W : 342.78
SMILES Code : O=C(O)[C@@H](NC(C1=CC=C(Cl)C=C1)=O)CC2=CNC3=C2C=CC=C3
Synonyms :
Benzotriptum
MDL No. :MFCD00069302

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