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Chemical Structure| 4122-68-3 Chemical Structure| 4122-68-3

Structure of 4122-68-3

Chemical Structure| 4122-68-3

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Product Citations

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 [ 4122-68-3 ]

CAS No. :4122-68-3
Formula : C8H6Cl2O2
M.W : 205.04
SMILES Code : O=C(Cl)COC1=CC=C(Cl)C=C1
MDL No. :MFCD00000727
InChI Key :VRBVHQUSAOKVDH-UHFFFAOYSA-N
Pubchem ID :77771

Safety of [ 4122-68-3 ]

GHS Pictogram:
Signal Word:Danger
Hazard Statements:H314
Precautionary Statements:P280-P305+P351+P338-P310
Class:8
UN#:3265
Packing Group:

Application In Synthesis of [ 4122-68-3 ]

* 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 [ 4122-68-3 ]
  • Downstream synthetic route of [ 4122-68-3 ]

[ 4122-68-3 ] Synthesis Path-Upstream   1~1

  • 1
  • [ 4122-68-3 ]
  • [ 223576-64-5 ]
References: [1] Tetrahedron Letters, 2015, vol. 56, # 29, p. 4383 - 4387.
 

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