A PKC inhibitor that displays immunosuppressive activity

Sotrastaurin – 5 mg

Brand:
Cayman
CAS:
425637-18-9
Storage:
-20
UN-No:
Non-Hazardous - /

Sotrastaurin is a protein kinase C (PKC) inhibitor that displays immunosuppressive activity, blocking T cell activation through the disruption of downstream NF-κB signaling.{27221,27224} In cell-free assays, sotrastaurin was reported to inhibit PKCα, βI, δ, ε, η, and θ 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/β-catenin signaling via the inhibition of glycogen synthase kinase 3 (IC50s = 229 and 172 nM for α and β isoforms, respectively), which is essential for embryogenesis and adult stem cell maintenance.{27225,27226}  

 

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Description

A PKC inhibitor that displays immunosuppressive activity, blocking T cell activation through the disruption of downstream NF-κB signaling; inhibits PKCα, βI, δ, ε, η, and θ with Ki values of 0.95, 0.64, 2.1, 3.2, 1.8, and 0.22 nM, respectively; also inhibits GSK3α and GSK3β (IC50s = 229 and 172 nM, respectively), which activates Wnt/β-catenin signaling and is important for adult stem cell maintenance

Formal name: 3-​​(1H-​​indol-​​3-​​yl)-​​4-​​[2-​​(4-​​methyl-​1-​​piperazinyl)-​​4-​​quinazolinyl]​-​1H-​pyrrole-​2,​5-​dione

Synonyms:  AEB071

Molecular weight: 438.5

CAS: 425637-18-9

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|GSK3||Product Type|Biochemicals|Kinase Inhibitors|PKC||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cell Biology|Cell Signaling|NF-κB Signaling||Research Area|Cell Biology|Cell Signaling|Wnt Signaling||Research Area|Cell Biology|Stem Cell Research||Research Area|Epigenetics, Transcription, & Translation|Transcription Factors||Research Area|Immunology & Inflammation|Adaptive Immunity||Research Area|Immunology & Inflammation|Allergy||Research Area|Immunology & Inflammation|Immunosuppressants||Research Area|Immunology & Inflammation|Innate Immunity

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