A highly selective

Bisindolylmaleimide I – 5 mg

Brand:
Cayman
CAS:
133052-90-1
Storage:
-20
UN-No:
Non-Hazardous - /

Bisindolylmaleimide I (BIM I) is a highly selective, cell-permeable, and reversible PKC inhibitor (Ki = 14 nM) that is structurally similar to the poorly selective PKC inhibitor staurosporine (Item No. 81590).{17275} It acts as a competitive inhibitor for the ATP binding site of PKC and shows high selectivity for PKCα, β1, β2, γ, δ, and ε isozymes. BIM I directly inhibits glycogen synthase kinase 3 (GSK3) in primary adipocyte lysates (IC50 = 360 nM) and in GSK3β immunoprecipitates derived from rat epididymal adipocytes (IC50 = 170 nM).{17379} It also competitively antagonizes the serotonin (5-HT) receptor subtype 5-HT3 with a Ki value of 61 nM.{17380}  

 

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Description

A highly selective, cell-permeable, and reversible PKC inhibitor (Ki = 14 nM); competitive inhibitor for the ATP binding site of PKC; highly selective for PKCα, β1, β2, γ, δ, and ε isozymes; inhibits GSK3 in primary adipocyte lysates (IC50 = 360 nM) and in GSK3β immunoprecipitates derived from rat epididymal adipocytes (IC50 = 170 nM); competitively antagonizes the 5-HT3 receptor with a Ki value of 61 nM,

Formal name: 3-[1-[3-(dimethylamino)propyl]-1H-indol-3-yl]-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione

Synonyms:  BIM I|GF 109203X|Gö 6850

Molecular weight: 412.5

CAS: 133052-90-1

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|GSK3||Product Type|Biochemicals|Kinase Inhibitors|PKC||Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cell Biology|Cell Signaling

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