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[ CAS No. 4876-14-6 ] {[proInfo.proName]}

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Chemical Structure| 4876-14-6
Chemical Structure| 4876-14-6
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Faisal Aziz ; Kanamata Reddy ; Virneliz Fernandez Vega , et al. DOI:

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 [ 4876-14-6 ]

CAS No. :4876-14-6 MDL No. :MFCD07787426
Formula : C12H13ClN2O3 Boiling Point : -
Linear Structure Formula :- InChI Key :MPTXVJCCTVAVNL-UHFFFAOYSA-N
M.W : 268.70 Pubchem ID :11514549
Synonyms :

Safety of [ 4876-14-6 ]

Signal Word:Warning Class:N/A
Precautionary Statements:P280-P305+P351+P338 UN#:N/A
Hazard Statements:H302 Packing Group:N/A
GHS Pictogram:

Application In Synthesis of [ 4876-14-6 ]

* 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.

  • Upstream synthesis route of [ 4876-14-6 ]
  • Downstream synthetic route of [ 4876-14-6 ]

[ 4876-14-6 ] Synthesis Path-Upstream   1~2

  • 1
  • [ 4900-38-3 ]
  • [ 4876-14-6 ]
Reference： [1] Chemical and Pharmaceutical Bulletin, 1985, vol. 33, # 9, p. 3775 - 3786
  • 2
  • [ 4876-10-2 ]
  • [ 4876-14-6 ]
Reference： [1] Chemical and Pharmaceutical Bulletin, 1985, vol. 33, # 9, p. 3775 - 3786
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