Sotrastaurin

Sotrastaurin

CAT N°: 16726
Price:

From 74.00 62.90

Sotrastaurin is a protein kinase C (PKC) inhibitor that displays immunosuppressive activity, blocking T cell activation through the disruption of downstream NF-?B signaling.{27221,27224} In cell-free assays, sotrastaurin was reported to inhibit PKC?, ?I, ?, ?, ?, and ? with Ki values of 0.95, 0.64, 2.1, 3.2, 1.8, and 0.22 nM, respectively.{27221} Sotrastaurin can prevent the production of various cytokines by activated T cells, macrophages, and keratinocytes in vitro and has been shown to inhibit an acute allergic contact dermatitis response in rats when dosed orally at 30 mg.{27223} However, clinical investigation of sotrastaurin for its potential to prevent renal transplant rejection was halted during phase II testing due to high incidence of rejection.{27222} Sotrastaurin is also reported to activate Wnt/?-catenin signaling via the inhibition of glycogen synthase kinase 3 (IC50s = 229 and 172 nM for ? and ? isoforms, respectively), which is essential for embryogenesis and adult stem cell maintenance.{27225,27226}

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • 3-(1H-indol-3-yl)-4-[2-(4-methyl-1-piperazinyl)-4-quinazolinyl]-1H-pyrrole-2,5-dione
  • Correlated keywords
    • 908351-31-5 1058706-32-3 immunosuppressant protein kinase C PKC T cell NF-?B cytokine immunology inhibitor transplant GSK3 glycogen synthase kinase 3 Wnt ?-catenin stem cell nuclear factor ? B signaling downstream cell-free assay PKC? PKC?I PKC? PKC? PKC? PKC? macrophages keratinocytes in vitro acute allergic contact dermatitis response rat oral dose renal kidney transplant rejection GSK3? GSK3? ? ? isoform embryogenesis adult AEB 071
  • Product Overview:
    Sotrastaurin is a protein kinase C (PKC) inhibitor that displays immunosuppressive activity, blocking T cell activation through the disruption of downstream NF-?B signaling.{27221,27224} In cell-free assays, sotrastaurin was reported to inhibit PKC?, ?I, ?, ?, ?, and ? with Ki values of 0.95, 0.64, 2.1, 3.2, 1.8, and 0.22 nM, respectively.{27221} Sotrastaurin can prevent the production of various cytokines by activated T cells, macrophages, and keratinocytes in vitro and has been shown to inhibit an acute allergic contact dermatitis response in rats when dosed orally at 30 mg.{27223} However, clinical investigation of sotrastaurin for its potential to prevent renal transplant rejection was halted during phase II testing due to high incidence of rejection.{27222} Sotrastaurin is also reported to activate Wnt/?-catenin signaling via the inhibition of glycogen synthase kinase 3 (IC50s = 229 and 172 nM for ? and ? isoforms, respectively), which is essential for embryogenesis and adult stem cell maintenance.{27225,27226}

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