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Chemical Structure| 90098-06-9 Chemical Structure| 90098-06-9

Structure of 90098-06-9

Chemical Structure| 90098-06-9

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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 [ 90098-06-9 ]

CAS No. :90098-06-9
Formula : C19H15ClN2O4
M.W : 370.79
SMILES Code : O=C1C=C(CC(C(O)=O)NC(C2=C(Cl)C=CC=C2)=O)C3=CC=CC=C3N1
MDL No. :MFCD30748223
InChI Key :CICRNAAVEZYNSB-UHFFFAOYSA-N
Pubchem ID :13342115

Safety of [ 90098-06-9 ]

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P280-P301+P312-P302+P352-P305+P351+P338

Application In Synthesis of [ 90098-06-9 ]

* All experimental methods are cited from the reference, please refer to the original source for details. We do not guarantee the accuracy of the content in the reference.

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